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List of works by Andrzej Bojarski

-Skatyltryptamines-Dual 5-HTR/DR Ligands with Antipsychotic and Procognitive Potential

scientific article published on 29 July 2021

1,2,3,4-tetrahydroisoquinoline derivatives: a new class of 5-HT1A receptor ligands

scientific article published on 01 February 1999

1-Aryl-4-(4-succinimidobutyl)piperazines and their conformationally constrained analogues: synthesis, binding to serotonin (5-HT1A, 5-HT2A, 5-HT7), alpha1-adrenergic, and dopaminergic D2 receptors, and in vivo 5-HT1A functional characteristics

scientific article

1-methyl-1,2,3,4-tetrahydroisoquinoline protects against rotenone-induced mortality and biochemical changes in rat brain

scientific article published in April 2003

11th German Conference on Chemoinformatics (GCC 2015) : Fulda, Germany. 8-10 November 2015.

scientific article (publication date: April 2016)

2-Aminoimidazole-based antagonists of the 5-HT6 receptor - A new concept in aminergic GPCR ligand design

scientific article published on 05 June 2019

5-HT1A receptor ligands and their therapeutic applications: review of new patents

scientific article published on 07 September 2018

7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands

scientific article published on 10 May 2007

8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone

scientific article

A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties

scientific article published on 22 August 2020

A linear combination of pharmacophore hypotheses as a new tool in search of new active compounds--an application for 5-HT1A receptor ligands

scientific article (publication date: 2013)

A multidimensional analysis of machine learning methods performance in the classification of bioactive compounds

article

A new class of 5-HT 1A receptor antagonists with procognitive and antidepressant properties

scientific article published in September 2021

A new class of arylpiperazine derivatives: the library synthesis on SynPhase lanterns and biological evaluation on serotonin 5-HT(1A) and 5-HT(2A) receptors

scientific article published in September 2004

A new crystal structure fragment-based pharmacophore method for G protein-coupled receptors

scientific article

A study on application of impregnated synthetic peptide TLC stationary phases for the screening of 5-HT1A ligands. Part 2.

scientific article

Active conformation of some arylpiperazine postsynaptic 5-HT(1A) receptor antagonists.

scientific article published in April 2002

Allosteric Inhibition of Serotonin 5-HT7 Receptors by Zinc Ions

scientific article

Aminergic GPCR-ligand interactions: A chemical and structural map of receptor mutation data

scientific article published on 27 November 2018

Amino Acid Hot Spots of Halogen Bonding: A Combined Theoretical and Experimental Case Study of the 5-HT7 Receptor

scientific article published on 21 September 2018

An Algorithm to Identify Target-Selective Ligands - A Case Study of 5-HT7/5-HT1A Receptor Selectivity

scientific article

An application of machine learning methods to structural interaction fingerprints--a case study of kinase inhibitors.

scientific article published on 10 December 2013

Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors

scientific article

Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT₁A receptor functional profile.

scientific article

Antidepressant-like activity of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and evidence for the involvement of serotonin receptor subtypes in their mechanism of action

scientific article published on 29 November 2015

Application of Structural Interaction Fingerpints (SIFts) into post-docking analysis - insight into activity and selectivity.

scientific article published on 22 March 2013

Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands

scientific article published on 29 September 2011

Arylpiperazine derivatives of 3-propyl-beta-tetralonohydantoin as new 5-HT1A and 5-HT2A receptor ligands.

scientific article

Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands

scientific article published on 3 May 2006

Arylpiperazinylalkyl derivatives of 8-amino-1,3-dimethylpurine-2,6-dione as novel multitarget 5-HT/D receptor agents with potential antipsychotic activity

scientific article published on 25 September 2015

Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

Asymmetric clustering index in a case study of 5-HT1A receptor ligands

scientific article (publication date: 2014)

Atomic diversity, molecular diversity, and chemical diversity: the concept of chemodiversity

scientific article published in August 2009

Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation

scientific article published on 8 February 2009

Bioisosteric matrices for ligands of serotonin receptors

scientific article published on 13 March 2015

Both stereoselective (R)- and (S)-1-Methyl-1,2,3,4-tetrahydroisoquinoline enantiomers protect striatal terminals against rotenone-induced suppression of dopamine release

scientific article

Comparison of an Addictive Potential of μ-Opioid Receptor Agonists with G Protein Bias: Behavioral and Molecular Modeling Studies

scientific article published on 27 December 2021

Concentration-Dependent Dual Mode of Zn Action at Serotonin 5-HT1A Receptors: In Vitro and In Vivo Studies

scientific article published on 12 December 2015

Conformational constraints on side chains in protein residues increase their information content

scientific article published on 01 November 2003

Conformational fluctuations versus constraints in amino acid side chains: the evolution of information content from free amino acids to proteins

scientific article published on 01 March 2006

Conformational restriction in novel NAN-190 and MP3022 analogs and their 5-HT(1A) receptor activity

scientific article published on 01 September 2006

Creating the New from the Old: Combinatorial Libraries Generation with Machine-Learning-Based Compound Structure Optimization

scientific article

Data-Driven Analysis of Fluorination of Ligands of Aminergic G Protein Coupled Receptors

scientific article published on 8 November 2021

Design and Synthesis of Novel Aminoalkanamides Targeting Neurodegeneration and Symptoms of Alzheimer’s Disease

scientific article published on 17 September 2021

Design, Synthesis and Biological Evaluation of Potent Antioxidant 1-(2,5-Dimethoxybenzyl)-4-arylpiperazines and N -Azolyl Substituted 2-(4-Arylpiperazin-1-yl)

Development of New Methods Needs Proper Evaluation-Benchmarking Sets for Machine Learning Experiments for Class A GPCRs

scientific article published on 22 November 2019

Dual 5-HT6 and D3 Receptor Antagonists in a Group of 1H-Pyrrolo[3,2-c]quinolines with Neuroprotective and Procognitive Activity

scientific article published on 02 April 2019

Electrospray mass spectrometric studies of noncovalent complexes of buspirone hydrochloride and other serotonin 5-HT(1A) receptor ligands containing arylpiperazine moieties

scientific article published in January 2003

Emulating Docking Results Using a Deep Neural Network: A New Perspective for Virtual Screening

scientific article published on 16 September 2020

Evaluation of different machine learning methods for ligand-based virtual screening.

scientific article published on 19 April 2011

Exploiting uncertainty measures in compounds activity prediction using support vector machines

scientific article published on 7 November 2014

Extremely Randomized Machine Learning Methods for Compound Activity Prediction.

scientific article published on 9 November 2015

Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands.

scientific article published on 10 May 2018

Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands

scientific article published on 24 March 2015

Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers

scientific article published on 11 March 2019

From Homology Models to a Set of Predictive Binding Pockets-a 5-HT1A Receptor Case Study

scientific article published on 05 January 2017

Fujita-Ban QSAR analysis and CoMFA study of quinoline antagonists of immunostimulatory CpG-oligodeoxynucleotides.

scientific article published on 29 September 2006

Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands

scientific article (publication date: 2015)

GPCRdb in 2018: adding GPCR structure models and ligands.

scientific article published on 16 November 2017

GPCRdb: an information system for G protein-coupled receptors

scientific article published on 6 December 2016

GPCRdb: an information system for G protein-coupled receptors.

scientific article published on 17 November 2015

GPCRdb: the G protein-coupled receptor database - an introduction

scientific article

Halogen bonding enhances activity in a series of dual 5-HT6/D2 ligands designed in a hybrid bioisostere generation/virtual screening protocol

scholarly article in RSC Advances, vol. 6 no. 60, 2016

Homology modeling of the serotonin 5-HT1A receptor using automated docking of bioactive compounds with defined geometry

scientific article published in January 2006

Homology modelling of metabotropic glutamate receptor 2.

scientific article published on 19 April 2011

How can fluorine directly and indirectly affect the hydrogen bonding in molecular systems? – A case study for monofluoroanilines

scientific article published in May 2021

Hydrogen Bonds with Fluorine in Ligand–Protein Complexes-the PDB Analysis and Energy Calculations

scientific article published on 2 February 2022

Identification of a Potent and Selective 5-HT<sub>1A</sub> Receptor Agonist with <i>In Vitro</i> and <i>In Vivo</i> Antinociceptive Activity

scientific article published on 02 December 2020

Identification of novel serotonin transporter compounds by virtual screening

scientific article published on 26 February 2014

Imidazolidine-4-one derivatives in the search for novel chemosensitizers of Staphylococcus aureus MRSA: synthesis, biological evaluation and molecular modeling studies.

scientific article published on 24 June 2015

Impact of template choice on homology model efficiency in virtual screening

scientific article

In Search of Effective Anticancer Agents-Novel Sugar Esters Based on Polyhydroxyalkanoate Monomers

scientific article published on 5 July 2021

In Silico Methods for the Discovery of Orthosteric GABA Receptor Compounds

In the search for a lead structure among series of potent and selective hydantoin 5-HT7 R agents: The drug-likeness in vitro study.

scientific article published on 8 September 2017

Introduction of a new complex imide system into the structure of LCAPs. The synthesis and a 5-HT1A, 5-HT2A and D2 receptor binding study.

scientific article published in November 2004

Ligand-Based Virtual Screening in a Search for Novel Anti-HIV-1 Chemotypes

scientific article published on 2 October 2015

Ligand-directed trafficking of receptor stimulus

scientific article

Ligand-guided homology modelling of the GABAB2 subunit of the GABAB receptor

scientific article

Low Basicity as a Characteristic for Atypical Ligands of Serotonin Receptor 5-HT2

scientific article published on 21 January 2021

Low-basicity 5-HT7 Receptor Agonists Synthesized Using the van Leusen Multicomponent Protocol

scientific article

Mass-spectrometric studies of new 6-nitroquipazines-serotonin transporter inhibitors

scientific article published on October 2011

Modification of the structure of 4, 6-disubstituted 2-(4-alkyl-1-piperazinyl)pyridines: synthesis and their 5-HT2A receptor activity.

scientific article published in April 2003

Molecular Modeling of µ Opioid Receptor Ligands with Various Functional Properties: PZM21, SR-17018, Morphine, and Fentanyl-Simulated Interaction Patterns Confronted with Experimental Data

scientific article published on 12 October 2020

Molecular mechanism of serotonin transporter inhibition elucidated by a new flexible docking protocol

scientific article

Molecules as complex adaptative systems: constrained molecular properties and their biochemical significance

scientific article

Multi-Step Protocol for Automatic Evaluation of Docking Results Based on Machine Learning Methods--A Case Study of Serotonin Receptors 5-HT(6) and 5-HT(7).

scientific article published on 8 April 2015

Multiple conformational states in retrospective virtual screening – homology models vs. crystal structures: beta-2 adrenergic receptor case study

scientific article (publication date: 2015)

N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile.

scientific article published on 30 November 2015

N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties

scientific article

NEW SPIROHYDANTOIN DERIVATIVES - SYNTHESIS, PHARMACOLOGICAL EVALUATION, AND MOLECULAR MODELING STUDY

scientific article published in November 2016

New 1-arylindoles based serotonin 5-HT7 antagonists. Synthesis and binding evaluation studies

scientific article published on 28 January 2014

New 8-aminoalkyl derivatives of purine-2,6-dione with arylalkyl, allyl or propynyl substituents in position 7, their 5-HT1A, 5-HT2A, and 5-HT7 receptor affinity and pharmacological evaluation

scientific article published in January 2013

New 9- or 10-arylpiperazinoalkyl substituted pyrimido- or diazepino[2,1-f]purines with partial or full 5-HT1A agonistic activity

New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation

scientific article published in May 2004

New arylpiperazines with flexible versus partly constrained linker as serotonin 5-HT(1A)/5-HT(7) receptor ligands

scientific article

New arylpiperazinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and dihydro[1,3]oxazolo[2,3-f]purinedione targeting the serotonin 5-HT1A /5-HT2A /5-HT7 and dopamine D2 receptors

scientific article

New imide 5-HT1A receptor ligands - modification of terminal fragment geometry

scientific article published on 28 February 2004

New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation

scientific article published in June 2010

New strategy for receptor-based pharmacophore query construction: a case study for 5-HT₇ receptor ligands

scientific article

Novel 1H-Pyrrolo[3,2-c]quinoline Based 5-HT6 Receptor Antagonists with Potential Application for the Treatment of Cognitive Disorders Associated with Alzheimer's Disease

scientific article

Novel 4-aryl-pyrido[1,2- c ]pyrimidines with dual SSRI and 5-HT 1A activity. Part 5

scientific article published on 09 May 2015

Novel 5-HT7R antagonists, arylsulfonamide derivatives of (aryloxy)propyl piperidines: Add-on effect to the antidepressant activity of SSRI and DRI, and pro-cognitive profile

scientific article published on 29 March 2017

Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT1A/5-HT7 receptor antagonists and phosphodiesterase 4/7 inhibitors with procognitive and antidepressant activity

scientific article published on 17 June 2020

Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation

scientific article published on 13 February 2007

Novel mannich bases, 5-arylimidazolidine-2,4-dione derivatives with dual 5-HT(1A) receptor and serotonin transporter affinity

scientific article published on 3 January 2013

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects

scientific article

Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.

scientific article published on 16 December 2017

Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.

scientific article published on 16 April 2015

Novel, flexible, and conformationally defined analogs of gepirone: synthesis and 5-HT1A, 5-HT2A, and D2 receptor activity.

scientific article published in February 2005

ONIOM and FMO-EDA study of metabotropic glutamate receptor 1: Quantum insights into the allosteric binding site

On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists

scientific article published on 01 December 1999

Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HT Receptor Ligands

scientific article published on 20 October 2018

PRELIMINARY EVALUATION OF CENTRAL NERVOUS SYSTEM ACTIVITY OF (E)-N-2-METHYL-3-PHENYLPROP-2-ENYL ((E)-N- α-METHYLCINNAMYL) DERIVATIVES OF SELECTED AMINOALKANOLS.

scientific article

Parallel solid-phase synthesis and characterization of new sulfonamide and carboxamide proline derivatives as potential CNS agents

scientific article

Pharmacophore models for metabotropic 5-HT receptor ligands

scientific article

Preliminary study on application of impregnated synthetic peptide TLC stationary phases for the pre-screening of 5-HT1A ligands.

scientific article

Prenatal Exposure to Benzophenone-3 Impairs Autophagy, Disrupts RXRs/PPARγ Signaling, and Alters Epigenetic and Post-Translational Statuses in Brain Neurons

scientific article published on 06 November 2018

Protective effect of 1-methyl-1,2,3,4-tetrahydroisoquinoline against dopaminergic neurodegeneration in the extrapyramidal structures produced by intracerebral injection of rotenone

scientific article published on 23 January 2004

Protein binding site analysis by means of structural interaction fingerprint patterns

scientific article published on 14 September 2011

Pyrano[2,3,4-cd]indole as a Scaffold for Selective Nonbasic 5-HT6R Ligands

scientific article

Pyrroloquinoline scaffold-based 5-HT 6 R ligands: Synthesis, quantum chemical and molecular dynamic studies, and influence of nitrogen atom position in the scaffold on affinity

scientific article published on 23 May 2018

Quinoline- and isoquinoline-sulfonamide analogs of aripiprazole: novel antipsychotic agents?

scientific article published on January 2014

Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation

scientific article published on 04 January 2012

Quinolinesulfonamides of aryloxy-/arylthio-ethyl piperidines: influence of an arylether fragment on 5-HT1A/5-HT7 receptor selectivity

scientific article published on 4 February 2013

Quo vadis G protein-coupled receptor ligands? A tool for analysis of the emergence of new groups of compounds over time

scientific article published on 2 December 2016

RECEPTOR AFFINITY AND PHOSPHODIESTERASES 4B AND 10A ACTIVITY OF OCTAHYDRO- AND 6,7-DIMETHOXY-3,4-DIHYDRO- ISOQUINOLIN-2(1H)-YL-ALKYL DERIVATIVES OF IMIDAZO- AND PYRIMIDINO[2,1-f]PURINES

Rapid binding site analysis by means of structural interaction fingerprint patterns – an implication to GPCR-targeted CADD.

scientific article published on 19 April 2011

Rational Design, Pharmacomodulation, and Synthesis of Dual 5-Hydroxytryptamine 7 (5-HT7)/5-Hydroxytryptamine 2A (5-HT2A) Receptor Antagonists and Evaluation by [(18)F]-PET Imaging in a Primate Brain

scientific article published on 8 September 2015

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation

scientific article published on 9 February 2016

Rational design of 5-HT 6 R ligands using a bioisosteric strategy: synthesis, biological evaluation and molecular modelling

scientific article published in 2015

Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT<sub>6</sub>R ligands binding mode

scientific article published on 09 October 2020

Reaction mechanism of sterol hydroxylation by steroid C25 dehydrogenase - Homology model, reactivity and isoenzymatic diversity

scientific article published on 27 April 2017

Receptor-based pharmacophores for serotonin 5-HT7R antagonists-implications to selectivity

scientific article published on 01 November 2006

Robust optimization of SVM hyperparameters in the classification of bioactive compounds

scientific article (publication date: 2015)

SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling

scientific article

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.

scientific article published on 18 March 2014

Salt Bridge in Ligand–Protein Complexes—Systematic Theoretical and Statistical Investigations

Search for a 5-CT alternative. In vitro and in vivo evaluation of novel pharmacological tools: 3-(1-alkyl-1H-imidazol-5-yl)-1H-indole-5-carboxamides, low-basicity 5-HT7 receptor agonists

scientific article published on 25 September 2018

Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs

scientific article published on 19 July 2018

Serotonin transporter and receptor ligands with antidepressant activity as neuroprotective and proapoptotic agents

scientific article published on 22 January 2017

Simulations in evolution. II. Relative fitness and the propagation of mutants

scientific article published on 01 March 2009

Simulations in evolution. III. Randomness as a generator of opportunities

scientific article published in January 2013

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one

scientific article published on 12 February 2015

Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands

scientific article

Sonication-Assisted Synthesis of(E)-2-Methyl-but-2-enyl Nucleoside Phosphonate Prodrugs

Spiro[pyrrolidine-3,3'-oxindoles] and Their Indoline Analogues as New 5-HT6 Receptor Chemotypes.

scientific article

Spiro[pyrrolidine-3,3'-oxindoles] as 5-HT7 receptor ligands

scientific article published on 12 June 2018

Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.

scientific article published on 6 May 2016

Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands.

scientific article

Structural insights into serotonin receptor ligands polypharmacology

scientific article published on 6 April 2018

Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.

scientific article published on 6 May 2016

Structure and spectral properties of β-carbolines. 8. Mechanism of the Pictet-Spengler cyclization: An MNDO approach

Structure-5-HT receptor affinity relationship in a new group of 7-arylpiperazynylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-amino-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione

scientific article published on 13 March 2015

Structure-5-HT/D2 Receptor Affinity Relationship in a New Group of 1-Arylpiperazynylalkyl Derivatives of 8-Dialkylamino-3,7-dimethyl-1H-purine-2,6(3H,7H)-dione.

scientific article published on 11 August 2016

Structure-activity relationship studies of CNS agents, Part 23: N-(3-phenylpropyl)- and N-[(E)-cinnamyl]-1,2,3,4-tetrahydroisoquinoline mimic 1-phenylpiperazine at 5-HT1A receptors

scientific article published on 01 July 1995

Structure-activity relationship studies of CNS agents, Part 25. 4,6-di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as new, potent 5-HT2A receptor ligands: a verification of the topographic model

scientific article published on 01 September 1995

Structure-activity relationship studies of CNS agents, XIX: Quantitative analysis of the alkyl chain effects on the 5-HT1A and 5-HT2 receptor affinities of 4-alkyl-1-arylpiperazines and their analogs

scientific article published on 01 February 1995

Structure-activity relationship studies of CNS agents, XXI: Two derivatives of 1-(o-methoxyphenyl)piperazine with an opposite function at 5-HT1A receptors

scientific article published on 01 April 1995

Structure-activity relationship studies of CNS agents--XVII. Spiro[piperidine-4',1-(1,2,3,4-tetrahydro-beta-carboline)] as a probe defining the extended topographic model of 5-HT1A receptors

scientific article published on 01 May 1995

Structure-activity relationship studies of CNS agents. Part 38. Novel 1,4-benzoxazin-3(4H)-one, 1,2-benzoxazolin-3-one and 1,3-benzoxazolin-2,4-dione arylpiperazine derivatives with different 5-HT1A and antagonistic 5-HT2A activities

scientific article published on 01 November 1999

Structure-activity relationship studies of CNS agents. Part 9: 5-HT1A and 5-HT2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines

scientific article published in April 1993

Structure-activity relationship studies of CNS agents. Part III. On the bioactive conformations of 1-arylpiperazines at 5-HT1A receptor

scientific article published on January 1, 1992

Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.

scientific article published in May 2015

Structure-intrinsic activity relationship studies in the group of 1-imido/amido substituted 4-(4-arylpiperazin-1-yl)cyclohexane derivatives; new, potent 5-HT1A receptor agents with anxiolytic- like activity.

scientific article published on 2 November 2005

Structure–activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT7 and 5-HT1A receptor ligands

scientific article published on 07 August 2014

Substitution mode of the amide fragment in some new N-[omega-[4-(2-methoxyphenyl)piperazin-1-yl]alkyl]pyrid-2(1H)-ones and their 5-HT1A/5-HT2A activity.

scientific article

Substructural Connectivity Fingerprint and Extreme Entropy Machines—A New Method of Compound Representation and Analysis

scientific article published on 23 May 2018

Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.

scientific article published on 13 June 2009

Synthesis and 5-HT(1A), 5-HT(2A) receptor activity of new beta-tetralonohydantoins

scientific article published in August 2005

Synthesis and Anticonvulsant Activity of N-(trans)- 3-phenylprop-2-en-1-yl (Cinnamyl) Derivatives of Aminoalkanols

scientific article published on 8 August 2014

Synthesis and Evaluation of Antidepressant-like Activity of Some 4-Substituted 1-(2-methoxyphenyl)Piperazine Derivatives

scientific article published on 14 August 2014

Synthesis and Structure-Activity Relationship Analysis of 5-HT₇ Receptor Antagonists: Piperazin-1-yl Substituted Unfused Heterobiaryls.

scientific article published on 31 March 2016

Synthesis and activity of substituted 2-phenylquinolin-4-amines, antagonists of immunostimulatory CpG-oligodeoxynucleotides

scientific article published in March 2003

Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect

scientific article published on 26 September 2019

Synthesis and biological evaluation of novel pyrrolidine-2,5-dione derivatives as potential antidepressant agents. Part 1.

scientific article

Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.

scientific article

Synthesis and pharmacological evaluation of new arylpiperazines. 3-[4-[4-(3-chlorophenyl)-1-piperazinyl]butyl]-quinazolidin-4-one - a dual serotonin 5-HT(1A)/5-HT(2A) receptor ligand with an anxiolytic-like activity

scientific article published in December 2002

Synthesis and serotonin receptor activity of the arylpiperazine alkyl/propoxy derivatives of new azatricycloundecanes

scientific article published on 8 April 2008

Synthesis and structural investigation of some pyrimido[5,4-c]quinolin-4(3H)-one derivatives with a long-chain arylpiperazine moiety as potent 5-HT(1A/2A) and 5-HT(7) receptor ligands

scientific article

Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT1A receptor ligands.

scientific article

Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.

scientific article published on 4 July 2008

Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT1A receptor ligands.

scientific article

Synthesis, anticonvulsant activity and 5-HT1A, 5-HT2A receptor affinity of new N-[(4-arylpiperazin-1-yl)-alkyl] derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione

scientific article published on 04 April 2006

Synthesis, anticonvulsant activity and 5-HT1A/5-HT7 receptors affinity of 1-[(4-arylpiperazin-1-yl)-propyl]-succinimides

scientific article published on 01 January 2012

Synthesis, anticonvulsant properties and 5-HT1A/5-HT2A receptor affinity of new N-[(4-arylpiperazin-1-yl)-propyl]-2-aza-spiro[4.4]nonane and [4.5]decane-1,3-dione derivatives.

scientific article published in May 2005

Synthesis, antidepressant evaluation and docking studies of long-chain alkylnitroquipazines as serotonin transporter inhibitors

scientific article published on 11 April 2013

Synthesis, in vitro and in vivo 5-HT1A/5-HT2A serotonin receptor activity of new hybrid 1,2,3,4-tetrahydro-gamma-carbolines with 1-(2-methoxyphenyl)piperazine moiety.

scientific article

Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors

scientific article

The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1,3,5-triazine

scientific article published on 13 April 2017

The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists

scientific article published on 6 March 2010

The effect of the intramolecular C-H⋯O interactions on the conformational preferences of bis-arylsulfones - 5-HT receptor antagonists and beyond

scientific article published on 17 May 2018

The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands

scientific article published in December 2004

The impact of the halogen bonding on D2 and 5-HT1A/5-HT7 receptor activity of azinesulfonamides of 4-[(2-ethyl)piperidinyl-1-yl]phenylpiperazines with antipsychotic and antidepressant properties.

scientific article published on 4 May 2017

The importance of template choice in homology modeling. A 5-HT6R case study

The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones

scientific article

The influence of hashed fingerprints density on the machine learning methods performance.

scientific article published on 22 March 2013

The influence of negative training set size on machine learning-based virtual screening

scientific article

The influence of substitution at aromatic part of 1,2,3,4-tetrahydroisoquinoline on in vitro and in vivo 5-HT(1A)/5-HT(2A) receptor activities of its 1-adamantoyloaminoalkyl derivatives

scientific article published in January 2002

The influence of the inactives subset generation on the performance of machine learning methods

scientific article

The influence of the negative-positive ratio and screening database size on the performance of machine learning-based virtual screening.

scientific article published on 6 April 2017

The influence of training actives/inactives ratio on machine learning performance

scholarly article by Rafał Kurczab et al published 2013 in Journal of Cheminformatics

The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists

scientific article

The salt bridge in ligand-protein complexes - systematic theoretical and statistical investigations

Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

scientific article published on 10 April 2013

Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.

scientific article published on 30 November 2015

Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.

scientific article published on 24 December 2014

Variation, natural selection, and information content--a simulation

scientific article published in October 2007

Virtual screening-driven discovery of dual 5-HT6/5-HT2A receptor ligands with pro-cognitive properties

scientific article published on 07 November 2019

mTOR activation by constitutively active serotonin6 receptors as new paradigm in neuropathic pain and its treatment

scientific article published on 05 June 2020

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