List of works - Paweł Zajdel

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

scientific article published on 05 June 2019

2-Phenyl-1 H -pyrrole-3-carboxamide as a New Scaffold for Developing 5-HT 6 Receptor Inverse Agonists with Cognition-Enhancing Activity

scientific article published on 11 March 2021

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

A New Highly Versatile Handle for Chemistry on a Solid Support: The Pipecolic Linker

article by Nicolas Masurier et al published 2 August 2012 in Chemistry—A European Journal

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 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 cytotoxic triterpene saponin from Lysimachia nummularia L.

scientific article published on 12 April 2013

A new highly versatile handle for chemistry on a solid support: the pipecolic linker

scientific article published in July 2010

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

scientific article

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

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

Application of the ring-closing metathesis to the formation of 2-aryl-1 H -pyrrole-3-carboxylates as building blocks for biologically active compounds

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

scientific article published on 29 September 2011

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

scientific article

Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity.

scientific article published on 10 September 2016

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

Biotransformation of 4-fluoro-N-(1-{2-[(propan-2-yl)phenoxy]ethyl}-8-azabicyclo[3.2.1]octan-3-yl)-benzenesulfonamide, a novel potent 5-HT7 receptor antagonist with antidepressant-like and anxiolytic properties: In vitro and in silico approach

scientific article published on 22 February 2018

ChemInform Abstract: Combinatorial Chemistry on Solid Support in the Search for Central Nervous System Agents

Combinatorial chemistry on solid support in the search for central nervous system agents

scientific article

Continuous flow ring-closing metathesis, an environmentally-friendly route to 2,5-dihydro-1H-pyrrole-3-carboxylates

article published in 2017

Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties

Determination of moxifloxacin and its oxidation products with kinetic evaluation under potassium permanganate treatment in acidic solution by ultra-performance liquid chromatography/tandem mass spectrometry.

scientific article published in November 2013

Directed solid-phase synthesis of trisubstituted imidazo[4,5-c]pyridines and imidazo[4,5-b]pyridines

scientific article published on 31 July 2014

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

Early 5-HT6 receptor blockade prevents symptom onset in a model of adolescent cannabis abuse

scientific article published on 24 April 2020

Ergotamine and nicergoline - facts and myths

scientific article

Imidazopyridine-Based 5-HT 6 Receptor Neutral Antagonists: Impact of N 1 -Benzyl and N 1 -Phenylsulfonyl Fragments on Different Receptor Conformational States

scientific article published on 13 January 2021

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases

scientific article published on 31 July 2019

Minor triterpene saponins from underground parts of Lysimachia thyrsiflora: structure elucidation, LC-ESI-MS/MS quantification, and biological activity

scientific article published on December 2013

N -(4-Arylpiperazinoalkyl)acetamide derivatives of 1,3- and 3,7-dimethyl-1 H -purine-2,6(3 H ,7 H )-diones and their 5-HT 6 , 5-HT 7 , and D 2 receptors affinity

scientific article published in February 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

Neuropathic pain-alleviating activity of novel 5-HT6 receptor inverse agonists derived from 2-aryl-1H-pyrrole-3-carboxamide

scientific article published in October 2021

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 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 imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases

scientific article published on 19 September 2020

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 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 antagonists of 5-HT and/or 5-HT receptors affect the brain monoamines metabolism and enhance the anti-immobility activity of different antidepressants in rats

scientific article published on 09 October 2018

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

scientific article

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

scientific article

Novel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation

scientific article published in January 2021

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

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

scientific article

Physical interaction between neurofibromin and serotonin 5-HT6 receptor promotes receptor constitutive activity.

scientific article published on 10 October 2016

Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

scientific article (publication date: September 2016)

Preliminary mutagenicity and genotoxicity evaluation of selected arylsulfonamide derivatives of (aryloxy)alkylamines with potential psychotropic properties.

scientific article published on 6 October 2015

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

Recycling the versatile Pipecolic linker

scientific article published on September 2010

Separation and characterization of ciprofloxacin, difloxacin, lomefloxacin, norfloxacin, and ofloxacin oxidation products under potassium permanganate treatment in acidic medium by UPLC-MS/MS.

scientific article

Solid-Phase Synthesis of Aryl-Alkylamine Derivatives Using Protected Aminoalcohol Building Blocks on SynPhaseTM Lanterns

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-phase synthetic route to multiple derivatives of a fundamental peptide unit.

scientific article

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

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

scientific article

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT and 5-HT Receptor Antagonist with Antipsychotic and Procognitive Properties

scientific article published on 23 September 2021

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

scientific article published on 13 June 2009

Sustainable synthesis of a potent and selective 5-HT7 receptor antagonist using a mechanochemical approach

scientific article published on 24 July 2020

Synthesis and 5-HT1A/5-HT2A activity of some butyl analogs in the group of phenylpiperazine alkyl pyrimido[2,1-f]theophyllines.

scientific article published in March 2005

Synthesis and Pharmacological Evaluation of Novel Silodosin-Based Arylsulfonamide Derivatives as α/α-Adrenergic Receptor Antagonist with Potential Uroselective Profile

scientific article published on 29 August 2018

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I.

scientific article published in June 2005

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 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 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 pipecolic linker—an acid-labile handle for derivatization of secondary amines on a solid-support. Part 3

article by Paweł Zajdel et al published February 2013 in Tetrahedron Letters

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

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

List of works by Paweł Zajdel

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

2-Phenyl-1 H -pyrrole-3-carboxamide as a New Scaffold for Developing 5-HT 6 Receptor Inverse Agonists with Cognition-Enhancing Activity

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

A New Highly Versatile Handle for Chemistry on a Solid Support: The Pipecolic Linker

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

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

A new cytotoxic triterpene saponin from Lysimachia nummularia L.

A new highly versatile handle for chemistry on a solid support: the pipecolic linker

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

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

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

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

Application of the ring-closing metathesis to the formation of 2-aryl-1 H -pyrrole-3-carboxylates as building blocks for biologically active compounds

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

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

Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity.

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

Biotransformation of 4-fluoro-N-(1-{2-[(propan-2-yl)phenoxy]ethyl}-8-azabicyclo[3.2.1]octan-3-yl)-benzenesulfonamide, a novel potent 5-HT7 receptor antagonist with antidepressant-like and anxiolytic properties: In vitro and in silico approach

ChemInform Abstract: Combinatorial Chemistry on Solid Support in the Search for Central Nervous System Agents

Combinatorial chemistry on solid support in the search for central nervous system agents

Continuous flow ring-closing metathesis, an environmentally-friendly route to 2,5-dihydro-1H-pyrrole-3-carboxylates

Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties

Determination of moxifloxacin and its oxidation products with kinetic evaluation under potassium permanganate treatment in acidic solution by ultra-performance liquid chromatography/tandem mass spectrometry.

Directed solid-phase synthesis of trisubstituted imidazo[4,5-c]pyridines and imidazo[4,5-b]pyridines

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

Early 5-HT6 receptor blockade prevents symptom onset in a model of adolescent cannabis abuse

Ergotamine and nicergoline - facts and myths

Imidazopyridine-Based 5-HT 6 Receptor Neutral Antagonists: Impact of N 1 -Benzyl and N 1 -Phenylsulfonyl Fragments on Different Receptor Conformational States

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases

Minor triterpene saponins from underground parts of Lysimachia thyrsiflora: structure elucidation, LC-ESI-MS/MS quantification, and biological activity

N -(4-Arylpiperazinoalkyl)acetamide derivatives of 1,3- and 3,7-dimethyl-1 H -purine-2,6(3 H ,7 H )-diones and their 5-HT 6 , 5-HT 7 , and D 2 receptors affinity

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

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

Neuropathic pain-alleviating activity of novel 5-HT6 receptor inverse agonists derived from 2-aryl-1H-pyrrole-3-carboxamide

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

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

New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases

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

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

Novel antagonists of 5-HT and/or 5-HT receptors affect the brain monoamines metabolism and enhance the anti-immobility activity of different antidepressants in rats

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

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

Novel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation

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

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

Physical interaction between neurofibromin and serotonin 5-HT6 receptor promotes receptor constitutive activity.

Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

Preliminary mutagenicity and genotoxicity evaluation of selected arylsulfonamide derivatives of (aryloxy)alkylamines with potential psychotropic properties.

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

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

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

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

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

Recycling the versatile Pipecolic linker

Separation and characterization of ciprofloxacin, difloxacin, lomefloxacin, norfloxacin, and ofloxacin oxidation products under potassium permanganate treatment in acidic medium by UPLC-MS/MS.

Solid-Phase Synthesis of Aryl-Alkylamine Derivatives Using Protected Aminoalcohol Building Blocks on SynPhaseTM Lanterns

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

Solid-phase synthetic route to multiple derivatives of a fundamental peptide unit.

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

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

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT and 5-HT Receptor Antagonist with Antipsychotic and Procognitive Properties

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

Sustainable synthesis of a potent and selective 5-HT7 receptor antagonist using a mechanochemical approach

Synthesis and 5-HT1A/5-HT2A activity of some butyl analogs in the group of phenylpiperazine alkyl pyrimido[2,1-f]theophyllines.

Synthesis and Pharmacological Evaluation of Novel Silodosin-Based Arylsulfonamide Derivatives as α/α-Adrenergic Receptor Antagonist with Potential Uroselective Profile

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I.

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.

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

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

The pipecolic linker—an acid-labile handle for derivatization of secondary amines on a solid-support. Part 3

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

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

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

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