A. Gomtsyan

发表

Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design.

S. C. Panchal, Philip B. Cox, P. Hajduk, 2020, Journal of medicinal chemistry.

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.

A. Gomtsyan, Jill M. Wetter, J. Sullivan, 2008, Journal of medicinal chemistry.

TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats

A. Gomtsyan, J. Segreti, Robert G. Schmidt, 2015, Temperature.

Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.

A. Gomtsyan, Chih-Hung Lee, E. Bayburt, 2011, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

A. Gomtsyan, Chih-Hung Lee, Robert G. Schmidt, 2010, Bioorganic & medicinal chemistry.

[3H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a Novel, Stereoselective, High-Affinity Antagonist Is a Useful Radioligand for the Human Transient Receptor Potential Vanilloid-1 (TRPV1) Receptor

A. Gomtsyan, Chih-Hung Lee, T. Neelands, 2007, Journal of Pharmacology and Experimental Therapeutics.

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.

A. Gomtsyan, R. Snyder, Chih-Hung Lee, 2005, Bioorganic & medicinal chemistry.

MOLECULAR RECOGNITION AND SELF-ASSEMBLY BY WEAK HYDROGEN BONDING : UNPRECEDENTED SUPRAMOLECULAR HELICATE STRUCTURES FROM DIAMINE/DIOL MOTIFS

A. Gomtsyan, S. Hanessian, S. Roelens, 1994 .

Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia

A. Gomtsyan, P. Mantyh, J. Sullivan, 2009, Pain.

Nonnucleoside inhibitors of adenosine kinase.

A. Gomtsyan, Chih-Hung Lee, 2004, Current pharmaceutical design.

Vanilloid receptor TRPV1 in drug discovery

A. Gomtsyan, C. Faltynek, 2010 .

Synthesis of methyl 3-amino-deoxy-d-alluronate

A. Gomtsyan, I. Kalvinsh, S. Belyakov, 1992 .

Targeting TRP channels: beyond TRPV1

A. Gomtsyan, A. Szallasi, 2015, Naunyn-Schmiedeberg's Archives of Pharmacology.

Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.

A. Gomtsyan, Jill M. Wetter, Chih-Hung Lee, 2007, Bioorganic & medicinal chemistry letters.

α‐Methylation at Benzylic Fragment of N‐Aryl‐N′‐benzyl Ureas Provides TRPV1 Antagonists with Better Pharmacokinetic Properties and Higher Efficacy in Inflammatory Pain Model.

A. Gomtsyan, 2007 .

Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.

A. Gomtsyan, Jill M. Wetter, J. Segreti, 2006, Bioorganic & Medicinal Chemistry.

A-425619 [1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a Novel Transient Receptor Potential Type V1 Receptor Antagonist, Relieves Pathophysiological Pain Associated with Inflammation and Tissue Injury in Rats

A. Gomtsyan, J. Sullivan, Chih-Hung Lee, 2005, Journal of Pharmacology and Experimental Therapeutics.

A-425619 [1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a Novel and Selective Transient Receptor Potential Type V1 Receptor Antagonist, Blocks Channel Activation by Vanilloids, Heat, and Acid

A. Gomtsyan, J. Sullivan, Chih-Hung Lee, 2005, Journal of Pharmacology and Experimental Therapeutics.

Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.

A. Gomtsyan, Jill M. Wetter, Chih-Hung Lee, 2005, Journal of medicinal chemistry.

Novel sequential process from N-methoxyamides and vinyl Grignard reagents: new synthesis of beta-aminoketones.

A. Gomtsyan, A Gomtsyan, C. Lee, 2001, The Journal of organic chemistry.

Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

A. Gomtsyan, J. Segreti, A. King, 2014, Journal of medicinal chemistry.

TRPV1 Receptors in the CNS Play a Key Role in Broad-Spectrum Analgesia of TRPV1 Antagonists

A. Gomtsyan, J. Sullivan, M. Decker, 2006, The Journal of Neuroscience.

a Novel Transient Receptor Potential Type V 1 Receptor Antagonist , Relieves Pathophysiological Pain Associated with Inflammation and Tissue Injury in Rats

A. Gomtsyan, J. Sullivan, Chih-Hung Lee, 2005 .

Pharmacology of Modality-Specific Transient Receptor Potential Vanilloid-1 Antagonists That Do Not Alter Body Temperature

A. Gomtsyan, P. Mantyh, J. Segreti, 2012, Journal of Pharmacology and Experimental Therapeutics.

Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2004, Bioorganic & medicinal chemistry letters.

The synthesis of enantiomerically pure, symmetrically substituted cyclopropane phosphonic acids — A constrained analog of the GABA antagonist phaclophen

A. Gomtsyan, S. Hanessian, L. Cantin, 1997 .

4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.

A. Gomtsyan, S. Muchmore, Chih-Hung Lee, 2007, Bioorganic & medicinal chemistry.

Asymmetric conjugate additions of chiral allyl- and crotylphosphonamide anions to .alpha.,.beta.-unsaturated carbonyl compounds: highly stereocontrolled access to vicinally substituted carbon centers and chemically asymmetrized chirons

A. Gomtsyan, S. Hanessian, A. Payne, 1993 .

Heterocycles in drugs and drug discovery

A. Gomtsyan, A. Gomtsyan, 2012, Chemistry of Heterocyclic Compounds.

Pyridopyrimidine analogues as novel adenosine kinase inhibitors.

A. Gomtsyan, S. Muchmore, M. Jarvis, 2001, Bioorganic & medicinal chemistry letters.

Asymmetric Synthesis of Enantiomerically Pure and Diversely Functionalized Cyclopropanes.

A. Gomtsyan, S. Hanessian, D. Andreotti, 1995 .

Highly stereocontrolled sequential asymmetric Michael addition reactions with cinnamate esters - generation of three and four contiguous stereogenic centers on seven-carbon acyclic motifs

A. Gomtsyan, S. Hanessian, 1994 .

Stereoselective Synthesis of a Dipyridyl Transient Receptor Potential Vanilloid-3 (TRPV3) Antagonist.

A. Gomtsyan, Robert G. Schmidt, P. Kym, 2016, The Journal of organic chemistry.

TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds’ pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development

A. A. Romanovsky, A. Gomtsyan, E. Pintér, 2018, Acta physiologica.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Bruce Clapham, Bin Li, A. Gomtsyan, 2016, Journal of medicinal chemistry.

A. Gomtsyan, S. Hanessian, A. Payne, 1994 .

Pharmacology of Modality-Specific TRPV1 Antagonists That Do Not Alter Body Temperature

A. Gomtsyan, P. Mantyh, J. Segreti, 2012 .

Design, Synthesis, and Structure−Activity Relationship of 6-Alkynylpyrimidines as Potent Adenosine Kinase Inhibitors

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2002 .

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties. II. In vivo characterization in the rat.

A. Gomtsyan, E. Schweitzer, M. Williams, 2000, The Journal of pharmacology and experimental therapeutics.

Novel Approaches to Cross-linking High Molecular Weight Polysaccharides: Application to Guar-based Hydraulic Fracturing Fluids

H. D. Silva, P. Coveney, A. Gomtsyan, 2000 .

TRPV3 modulates nociceptive signaling through peripheral and supraspinal sites in rats.

A. Gomtsyan, Jill-Desiree Brederson, Robert G. Schmidt, 2017, Journal of neurophysiology.

(R)-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) Blocks Polymodal Activation of Transient Receptor Potential Vanilloid 1 Receptors in Vitro and Heat-Evoked Firing of Spinal Dorsal Horn Neurons in Vivo

A. Gomtsyan, J. Sullivan, Chih-Hung Lee, 2008, Journal of Pharmacology and Experimental Therapeutics.

In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.

A. Gomtsyan, Jill M. Wetter, Chih-Hung Lee, 2007, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of 5-heteroatom-substituted pyridopyrimidines as adenosine kinase inhibitors.

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2003, European journal of medicinal chemistry.

Synthesis and Structure—Activity Relationships of 5-Heteroatom-Substituted Pyridopyrimidines as Adenosine Kinase Inhibitors.

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2003 .

Clinical and Preclinical Experience with TRPV1 Antagonists as Potential Analgesic Agents

A. Gomtsyan, Jill-Desiree Brederson, J. Brederson, 2015 .

Design of adenosine kinase inhibitors from the NMR-based screening of fragments.

Jean M. Severin, E A Kowaluk, P. Hajduk, 2000, Journal of medicinal chemistry.

Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.

Jean M. Severin, A. Gomtsyan, S. Muchmore, 2006, Journal of Medicinal Chemistry.

A. Gomtsyan, J. Sullivan, Chih-Hung Lee, 2008, Journal of Pharmacology and Experimental Therapeutics.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

A. Gomtsyan, J. Segreti, R. Henry, 2016, Journal of medicinal chemistry.

TRPV3 modulates nociceptive signaling through peripheral and supraspinal sites in rats.

A. Gomtsyan, Robert G. Schmidt, P. Kym, 2017, Journal of neurophysiology.

Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models.

A. Gomtsyan, Robert G. Schmidt, P. Honore, 2009, The journal of pain : official journal of the American Pain Society.