Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors

Jun, Mi Ae; Park, Woul Seong; Kang, Seung Kyu; Kim, Ki Young; Kim, Kwang Rok; Dal Rhee, Sang; Bae, Myung Ae; Kang, Nam Sook; Sohn, Sang-Kwon; Kim, Sung Gyu; Lee, Jie Oh; Lee, Duck Hyung; Cheon, Hyae Gyeong; Kim, Sung Soo; Ahn, Jin Hee

doi:10.1016/j.ejmech.2007.11.029

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Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors

Jun, Mi Ae;
Park, Woul Seong;
Kang, Seung Kyu;
Kim, Ki Young;
Kim, Kwang Rok;
... Lee, Duck Hyung;
외 9명

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32

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34

초록

A series of pyrazoline derivatives with beta-amino acyl group were synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV. Several pyrazoline derivatives exhibited submicromolar inhibitory activities against DPP-IV. X-ray co-crystal structure of initial hit compound 1h was determined. Among this series, carboxylic acid substituted pyrazoline derivative 2u was the most active and greatly decreased the inhibitory activity toward CYP3A4 enzyme. (C) 2007 Elsevier Masson SAS. All rights reserved.

키워드

Dipeptidyl peptidase IV inhibitior; Pyrazoline; Anti-diabetic agent; GLUCAGON-LIKE PEPTIDE-1; GLUCOSE-TOLERANCE; POTENT; DERIVATIVES; PHARMACOKINETICS; DISCOVERY

제목: Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors

저자: Jun, Mi Ae; Park, Woul Seong; Kang, Seung Kyu; Kim, Ki Young; Kim, Kwang Rok; Dal Rhee, Sang; Bae, Myung Ae; Kang, Nam Sook; Sohn, Sang-Kwon; Kim, Sung Gyu; Lee, Jie Oh; Lee, Duck Hyung; Cheon, Hyae Gyeong; Kim, Sung Soo; Ahn, Jin Hee

DOI: 10.1016/j.ejmech.2007.11.029

발행일: 2008-09

유형: Article

저널명: European Journal of Medicinal Chemistry

권: 43

호: 9

페이지: 1889 ~ 1902