Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore

Autor:	Hiroyuki Nakahira, Yukihiro Nishio, Mutsuko Sakai, Michiko Ono, Shinya Tosaki, Eiji Sugaru, Masakuni Horiguchi, Hidenori Kimura, Tsutomu Nakagawa, Yumi Masui
Rok vydání:	2010
Předmět:	Molecular model Stereochemistry Dipeptidyl Peptidase 4 Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Stereoisomerism Pyrimidinones Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Piperidines Drug Discovery Animals Humans Moiety Structure–activity relationship Molecular Biology Dipeptidyl peptidase-4 Dipeptidyl-Peptidase IV Inhibitors Chemistry Organic Chemistry Rats Microsomes Liver Molecular Medicine Piperidine Pharmacophore
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:7246-7249
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2010.10.101
Popis:	Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0754dc268cbfd798fb76bb8881582b26 https://doi.org/10.1016/j.bmcl.2010.10.101 Zobrazit plný text záznamu Full Text from ScienceDirect