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List of works by Carlos Fraga

(2E)-N'-[(E)-2-Hy-droxy-benzyl-idene]-3-phenyl-prop-2-enohydrazide

scientific article

(2E)-N'-[(E)-Benzyl-idene]-3-phenyl-prop-2-enohydrazide from synchrotron radiation

scientific article

1-Methyl-7-(4-nitro-phen-yl)-3-phenyl-pyrazolo[3,4-b]pyrrolo[3,4-d]pyridine-6,8(3H,7H)-dione.

scientific article published on 13 November 2008

A novel Ca2+ channel antagonist reverses cardiac hypertrophy and pulmonary arteriolar remodeling in experimental pulmonary hypertension

scientific article

A proposed molecular basis for the selective resveratrol inhibition of the PGHS-1 peroxidase activity

scientific article published in November 2005

Acylhydrazone derivatives: a patent review

scientific article published on 12 September 2014

Adenosine A2A receptor agonist prevents cardiac remodeling and dysfunction in spontaneously hypertensive male rats after myocardial infarction

scientific article published on 06 March 2017

An Unusual Intramolecular Halogen Bond guides Conformational Selection.

scientific article

Anti-atherogenic effects of a new thienylacylhydrazone derivative, LASSBio-788, in rats fed a hypercholesterolemic diet

scientific article published on 7 September 2013

Antihyperalgesic effects of a novel muscarinic agonist (LASSBio-873) in spinal nerve ligation in rats

scientific article published in July 2013

Antihypertensive profile of 2-thienyl-3,4-methylenedioxybenzoylhydrazone is mediated by activation of the A2A adenosine receptor.

scientific article published on 7 July 2012

Antinociceptive profile of 2,3,6-trisubstituted piperidine alkaloids: 3-O-acetyl-spectaline and semi-synthetic derivatives of (-)-spectaline

scientific article

Antiplatelet properties of novel N-substituted-phenyl-1,2,3-triazole-4-acylhydrazone derivatives

scientific article published in May 2003

Antiprotozoal activity of (E)-cinnamic N-acylhydrazone derivatives

scientific article published on 5 December 2014

Beneficial effects of a novel agonist of the adenosine A2A receptor on monocrotaline-induced pulmonary hypertension in rats.

scientific article published on July 2013

Biotransformation of LASSBio-579 and pharmacological evaluation of p -hydroxylated metabolite a N -phenylpiperazine antipsychotic lead compound

scientific article published on 20 August 2012

CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline

scientific article

Cardiovascular effects induced by N-(4'-dihydro)-piperoylthiomorpholine in normotensive rats

scientific article published on 4 October 2010

Characterization of amide bond conformers for a novel heterocyclic template of N-acylhydrazone derivatives

scientific article published on 25 September 2013

Characterization of the conformational ensemble from bioactive N-acylhydrazone derivatives

scientific article published on 30 October 2009

Chiral gas chromatographic separation of 2-oxabicyclo[3.3.0]octane derivatives and their synthetic precursors

scientific article published in July 2000

Chiral separation of gamma-butyrolactone derivatives by gas chromatography on 2,3-di-O-methyl-6-O-tert.-butyldimethylsilyl-beta-cyclodextrin

scientific article

Combination of docking, molecular dynamics and quantum mechanical calculations for metabolism prediction of 3,4-methylenedioxybenzoyl-2-thienylhydrazone

article

Design and synthesis of 3,4-methylenedioxy-6-nitrophenoxyacetylhydrazone derivatives obtained from natural safrole: new lead-agents with analgesic and antipyretic properties

scientific article published on 10 August 2006

Design and synthesis of novel potent antinociceptive agents: methyl-imidazolyl N-acylhydrazone derivatives

scientific article published on 01 September 2000

Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.

scientific article published on 10 March 2010

Design, Synthesis, Experimental and Theoretical Characterization of a New Multitarget 2-Thienyl--Acylhydrazone Derivative

scientific article published in November 2018

Design, Synthesis, and Pharmacological Evaluation of First-in-Class Multitarget N-Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors

scientific article published on 17 February 2020

Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors

scientific article published on 24 December 2015

Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH)

scientific article published on 18 July 2009

Design, synthesis and antiinflammatory activity of novel phthalimide derivatives, structurally related to thalidomide

scientific article

Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents

scientific article published in January 2002

Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands

scientific article published in November 2003

Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors

scientific article

Design, synthesis, and pharmacological evaluation of new neuroactive pyrazolo[3,4-b]pyrrolo[3,4-d]pyridine derivatives with in vivo hypnotic and analgesic profile

scientific article

Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors

scientific article

Determination of the cardioactive prototype LASSBio-294 and its metabolites in dog plasma by LC–MS/MS: Application for a pharmacokinetic study

scientific article published on 03 March 2011

Development and validation of a LC-MS/MS method with electrospray ionization for determination of LASSBio-579 in rat plasma

scientific article published on 18 September 2006

Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors

scientific article published on 3 February 2009

Development of new CoMFA and CoMSIA 3D-QSAR models for anti-inflammatory phthalimide-containing TNFalpha modulators

scientific article

Different mol-ecular conformations in the crystal structures of three 5-nitro-imidazolyl derivatives.

scientific article published on 23 February 2018

Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-Adrenergic receptor blocking properties

scientific article published on 16 April 2011

Discovery of Novel Orally Active Tetrahydro-Naphthyl-N-Acylhydrazones with In Vivo Anti-TNF-α Effect and Remarkable Anti-Inflammatory Properties

scientific article (publication date: 2016)

Discovery of naphthyl-N-acylhydrazone p38α MAPK inhibitors with in vivo anti-inflammatory and anti-TNF-α activity.

scientific article published on 17 August 2017

Discovery of novel orally active anti-inflammatory N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that inhibit TNF-α production

scientific article

Drug hybridization strategies: before or after lead identification?

scientific article published on 6 May 2009

Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases

scientific article published on 06 May 2019

Evaluating the prophylactic potential of the phtalimide derivative LASSBio 552 on allergen-evoked inflammation in rats.

scientific article published in March 2005

Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor.

scientific article published on 4 June 2019

Filtering promiscuous compounds in early drug discovery: is it a good idea?

scientific article published on 12 February 2016

From nature to drug discovery: the indole scaffold as a 'privileged structure'.

scientific article published on June 2009

Gastroprotective effects of N-acylarylhydrazone derivatives on ethanol-induced gastric lesions in mice are dependent on the NO/cGMP/KATP pathway

scientific article published on 03 September 2019

Histone deacetylases as targets for the treatment of neurodegenerative disorders: Challenges and future opportunities

scientific article published on 26 June 2020

Identification of novel functionalized carbohydrazonamides designed as Chagas disease drug candidates

scientific article published on 26 June 2019

Impairment of locomotor activity induced by the novel N-acylhydrazone derivatives LASSBio-785 and LASSBio-786 in mice

scientific article published on 19 March 2013

Improvement of enantioselective syntheses and chiral high resolution gas chromatographic analyses of (+)-2-allyl-2-carboethoxy-cyclopentanol

scientific article published on 01 January 1997

In vivo effect of LASSBio-785, a lipid-lowering and anti-inflammatory agent, on cardiac Ca(2+)-ATPases from hypercholesterolemic rats.

scientific article

Introduction to celebrating Latin American talent in chemistry

scientific article published in 2021

LASSBio-1135: a dual TRPV1 antagonist and anti-TNF-alpha compound orally effective in models of inflammatory and neuropathic pain

scientific article (publication date: 2014)

LASSBio-1422: a new molecular scaffold with efficacy in animal models of schizophrenia and disorders of attention and cognition

scientific article published on 13 October 2016

LASSBio-1425, an analog of thalidomide, decreases triglyceride and increases HDL cholesterol levels by inhibition of TNF-α production

scientific article published on 25 September 2015

LASSBio-1829 Hydrochloride: Development of a New Orally Active N-Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties.

scientific article

LASSBio-294, A compound with inotropic and lusitropic activity, decreases cardiac remodeling and improves Ca²(+) influx into sarcoplasmic reticulum after myocardial infarction

scientific article published on 29 July 2010

LASSBio-579, a prototype antipsychotic drug, and clozapine are effective in novel object recognition task, a recognition memory model

scientific article

LASSBio-881: an N-acylhydrazone transient receptor potential vanilloid subfamily type 1 antagonist orally effective against the hypernociception induced by capsaicin or partial sciatic ligation

scientific article

LASSBio-897 Reduces Lung Injury Induced by Silica Particles in Mice: Potential Interaction with the A2A Receptor

scientific article published on 31 October 2017

MAOS and medicinal chemistry: some important examples from the last years.

scientific article

Medicinal chemistry of N-acylhydrazones: new lead-compounds of analgesic, antiinflammatory and antithrombotic drugs

scientific article published on 01 January 2006

Microwave-assisted synthesis and structure-activity relationships of neuroactive pyrazolo[3,4-b]pyrrolo[3,4-d]pyridine derivatives

scientific article published on 16 November 2009

Molecular hybridization: a useful tool in the design of new drug prototypes

scientific article published on January 2007

N-Acylhydrazones as drugs

scientific article published on 09 July 2018

N-acylhydrazone derivative ameliorates monocrotaline-induced pulmonary hypertension through the modulation of adenosine AA2R activity

scientific article published on 24 February 2014

N-acylhydrazone improves exercise intolerance in rats submitted to myocardial infarction by the recovery of calcium homeostasis in skeletal muscle

scientific article published on 21 November 2013

NF-κB-IKKβ pathway as a target for drug development: realities, challenges and perspectives.

scientific article published on 19 February 2018

NSAIDs revisited: putative molecular basis of their interactions with peroxisome proliferator-activated gamma receptor (PPARgamma)

scientific article published on 14 December 2007

New anti-Alzheimer drugs from biodiversity: the role of the natural acetylcholinesterase inhibitors

scientific article

New class of potent antinociceptive and antiplatelet 10H-phenothiazine-1-acylhydrazone derivatives

scientific article

New insights into pharmacological profile of LASSBio-579, a multi-target N-phenylpiperazine derivative active on animal models of schizophrenia

scientific article published on 19 September 2012

New isoxazole derivatives designed as nicotinic acetylcholine receptor ligand candidates

scientific article published in February 2002

New optimized piperamide analogues with potent in vivo hypotensive properties

scientific article published in December 2004

New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

scientific article published in July 2005

Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: orally effective anti-inflammatory drug candidates

scientific article published on 25 December 2008

Novel agonist of adenosine receptor induces relaxation of corpus cavernosum in guinea pigs: an in vitro and in vivo study.

scientific article published in May 2015

Novel furfurylidene N-acylhydrazones derived from natural safrole: discovery of LASSBio-1215, a new potent antiplatelet prototype

scientific article published on 25 May 2011

Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists

scientific article published in June 2002

Novel potent imidazo[1,2-a]pyridine-N-Glycinyl-hydrazone inhibitors of TNF-α production: in vitro and in vivo studies

scientific article

Novel thienylacylhydrazone derivatives inhibit platelet aggregation through cyclic nucleotides modulation and thromboxane A2 synthesis inhibition

scientific article published on 20 April 2010

Partial agonism and fast dissociation of LASSBio-579 at dopamine D2 receptor

scientific article published on 17 April 2015

Pharmacokinetic evaluation of LASSBio-579: an N-phenylpiperazine antipsychotic prototype

scientific article published in June 2008

Pharmacokinetics and tissue distribution of a new heterocyclic N-phenylpiperazine derivative (LASSBio-581) in rats

scientific article published in October 2005

Pharmacological characterization of (3-thienylidene)-3,4-methylenedioxybenzoylhydrazide: a novel muscarinic agonist with antihypertensive profile

scientific article published on 3 December 2009

Phenylpiperazine derivatives: a patent review (2006 - present).

scientific article published on 07 September 2012

Privileged structures: a useful concept for the rational design of new lead drug candidates

scientific article

Proposal of a new PAF pharmacophoric map by the AM1 method

scientific article published on 01 August 1999

ROCK inhibition with Fasudil induces beta-catenin nuclear translocation and inhibits cell migration of MDA-MB 231 human breast cancer cells.

scientific article

Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.

scientific article

Sedation and antinociception induced by a new pyrazolo[3,4-b]pyrrolo[3,4-d]pyridine derivative (LASSBio-873) is modulated by activation of muscarinic receptors.

scientific article published on 24 July 2009

Serotonergic neurotransmission mediates hypothermia induced by the N-phenylpiperazine antipsychotic prototypes LASSBio-579 and LASSBio-581.

scientific article

Structural basis for the agonist action at free fatty acid receptor 1 (FFA1R or GPR40).

scientific article

Structural insights into IKKbeta inhibition by natural products staurosporine and quercetin

scientific article published on 22 October 2009

Structure-based prediction and biosynthesis of the major mammalian metabolite of the cardioactive prototype LASSBio-294

scientific article published on 21 April 2010

Studies on antiplatelet agents from natural safrole. II. Synthesis and pharmacological properties of novel functionalized oxime O-benzylether derivatives

scientific article published on 01 December 1999

Studies toward the structural optimization of new brazilizone-related trypanocidal 1,3,4-thiadiazole-2-arylhydrazone derivatives

scientific article published on 18 September 2007

Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives

scientific article published on 08 May 2009

Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole

scientific article published on 9 August 2009

Synthesis and analgesic profile of novel N-containing heterocycle derivatives: arylidene 3-phenyl-1,2,4-oxadiazole-5-carbohydrazide

scientific article published on 01 November 1999

Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues

scientific article

Synthesis and anti-platelet activity of novel arylsulfonate--acylhydrazone derivatives, designed as antithrombotic candidates

scientific article published on 14 April 2007

Synthesis and antiplatelet evaluation of novel aryl-sulfonamide derivatives, from natural safrole

scientific article published on 01 June 1999

Synthesis and antitrypanosomal profile of new functionalized 1,3,4-thiadiazole-2-arylhydrazone derivatives, designed as non-mutagenic megazol analogues

scientific article published in December 2004

Synthesis and biological evaluation of new imidazo[1,2-a]pyridine derivatives designed as mefloquine analogues

scientific article published in October 2002

Synthesis and characterization of the atropisomeric relationships of a substituted N-phenyl-bipyrazole derivative with anti-inflammatory properties

scientific article published on 28 April 2012

Synthesis and pharmacological evaluation of a new class of bicyclic phospholipids, designed as platelet activating factor antagonists

scientific article published on 01 May 1998

Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.

scientific article published on 30 May 2013

Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole.

scientific article

Synthesis and pharmacological evaluation of novel antinociceptive N-substituted-phenylimidazolyl-4-acylhydrazone derivatives

scientific article published on 01 December 2002

Synthesis and pharmacological evaluation of novel isoquinoline N-sulphonylhydrazones designed as ROCK inhibitors

scientific article published on 01 December 2018

Synthesis and trypanocidal activity of novel 2,4,5-triaryl-N-hydroxylimidazole derivatives.

scientific article published on 15 March 2013

Synthesis and vasodilatory activity of new N-acylhydrazone derivatives, designed as LASSBio-294 analogues

scientific article published in May 2005

Synthesis, pharmacological evaluation and docking studies of new sulindac analogues

scientific article published on 6 December 2008

Synthesis, pharmacological evaluation and electrochemical studies of novel 6-nitro-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives: Discovery of LASSBio-881, a new ligand of cannabinoid receptors.

scientific article published on 17 January 2007

The Chalcone Lonchocarpin Inhibits Wnt/β-Catenin Signaling and Suppresses Colorectal Cancer Proliferation

scientific article published on 07 December 2019

The Use of Conformational Restriction in Medicinal Chemistry

scientific article published on 01 January 2019

The methylation effect in medicinal chemistry.

scientific article published on June 2011

The molecular basis for coxib inhibition of p38alpha MAP kinase

scientific article published in August 2005

The novel piperazine-containing compound LQFM018: Necroptosis cell death mechanisms, dopamine D4 receptor binding and toxicological assessment.

scientific article published on 23 March 2018

Treatment with Adenosine Receptor Agonist Ameliorates Pain Induced by Acute and Chronic Inflammation.

scientific article

Validated HPLC method for determination of LASSBio-581, a new heterocyclic N-phenylpiperazine derivative, in rat plasma

scientific article

Vasodilator and antihypertensive effects of a novel N-acylhydrazone derivative mediated by the inhibition of L-type Ca²⁺ channels

scientific article published on 7 September 2012