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

Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, +20

Journal of Medicinal Chemistry

Pain MedicineImmunologyReceptor AntagonistsNeuropathic PainMolecular Pain +16

A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model

Pamela S. Puttfarcken, Ping Han, Shailen K. Joshi, +13

Pain

Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists

Brian S. Brown, Ryan G. Keddy, Guo Zhu Zheng, +11

Bioorganic & Medicinal Chemistry

BiochemistryFunctional SelectivityMedicineReceptor (Biochemistry)Pharmacology +1

Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity

Guo Zhu Zheng, Yue Mao, Chih‐Hung Lee, +16

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyPyridopyrimidine DerivativesMolecular PhysiologyBiochemistryFunctional Selectivity +7

Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists

Robert G. Schmidt, Erol K. Bayburt, Steven P. Latshaw, +11

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryMedicinePharmacotherapyPharmacology +3

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

Richard J. Perner, John R. Koenig, Stanley DiDomenico, +11

Bioorganic & Medicinal Chemistry

MedicineDrug DiscoveryPharmacological AgentPharmacotherapyBiological Evaluation +3

Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis

Marc J. C. Scanio, Xenia B. Searle, Bo Liu, +19

ACS Medicinal Chemistry Letters

Pyridopyrimidine analogues as novel adenosine kinase inhibitors

Guo Zhu Zheng, Chih-Hung Lee, John K. Pratt, +20

Bioorganic & Medicinal Chemistry Letters

BiochemistryPyridopyrimidine AnaloguesMedicinePharmacological AgentPharmacotherapy +3

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

Arthur Gomtsyan, Erol K. Bayburt, Ryan G. Keddy, +14

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyAnti-inflammatoryHealth SciencesMedicinePain Medicine +10

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

Irene Drizin, Arthur Gomtsyan, Erol K. Bayburt, +7

Bioorganic & Medicinal Chemistry

Molecular PharmacologyDiversity Oriented SynthesisStructure–activity StudiesBiochemistryMedicine +6