Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin

Autor:	Joseph K. Wu, George J. Eiermann, Jeffrey T. Kuethe, Robert R. Wilkening, Aleksandr Petrov, Xiaohua Li, Ann E. Weber, Jason M. Cox, Ping Chen, Tesfaye Biftu, Kathryn A. Lyons, Joseph M. Metzger, Dennis Feng, Huaibing He, Ying-Duo Gao, Youwei Yan, James M. Apgar, Shiyao Xu, Ranabir Sinha Roy, Giovanna Scapin, Xiaoxia Qian, George A. Doss
Rok vydání:	2015
Předmět:	Stereochemistry Dipeptidyl Peptidase 4 Clinical Biochemistry Pharmaceutical Science Omarigliptin Biochemistry Heterocyclic Compounds 2-Ring chemistry.chemical_compound Structure-Activity Relationship Dogs Amide Drug Discovery Structure–activity relationship Animals Molecular Biology Dipeptidyl-Peptidase IV Inhibitors Pyrans chemistry.chemical_classification Sulfonamides Binding Sites Organic Chemistry Amides Sulfonamide Protein Structure Tertiary Rats Molecular Docking Simulation Orally active Long acting chemistry Molecular Medicine Half-Life
Zdroj:	Bioorganicmedicinal chemistry letters. 25(24)
ISSN:	1464-3405
Popis:	A series of novel substituted-[(3R)-amino-2-(2,5-difluorophenyl)]tetrahydro-2H-pyran analogs have been prepared and evaluated as potent, selective and orally active DPP-4 inhibitors. These efforts lead to the discovery of a long acting DPP-4 inhibitor, omarigliptin (MK-3102), which recently completed phase III clinical development and has been approved in Japan.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3841d78bae66cfd858b20702956053a6 https://pubmed.ncbi.nlm.nih.gov/26546218 Zobrazit plný text záznamu Full Text from ScienceDirect