상세 보기
Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents
- Kwak, Hyun Jung;
- Pyun, Yu Mi;
- Kim, Ji Young;
- Pagire, Haushabhau S.;
- Kim, Ki Young;
- ... Lee, Duck Hyung;
- 외 6명
Citations
WEB OF SCIENCE
41Citations
SCOPUS
42초록
A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. Among the benzimidazole series, compound 5k showed submicromolar in vitro activity toward human and mouse DGAT-1, good selectivity toward DGAT-2, human liver metabolic stability, and pharmacokinetic (PK) and safety profiles such as hERG, CYP and acute toxicity. Additionally, 5k showed good in vivo efficacy in 4 weeks study with DIO mouse model. (C) 2013 Elsevier Ltd. All rights reserved.
키워드
Diacylglycerol acyltransferase-1; DGAT-1; Triglycerides; TG; Obesity; Diabetes; Aminobenzimidazole; COA-DIACYLGLYCEROL ACYLTRANSFERASE; TRIGLYCERIDE SYNTHESIS; KEY ENZYME; OBESITY; MICE; IDENTIFICATION; INHIBITION; POTENT; DGAT1
- 제목
- Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents
- 저자
- Kwak, Hyun Jung; Pyun, Yu Mi; Kim, Ji Young; Pagire, Haushabhau S.; Kim, Ki Young; Kim, Kwang Rok; Dal Rhee, Sang; Jung, Won Hoon; Song, Jin Sook; Bae, Myung Ae; Lee, Duck Hyung; Ahn, Jin Hee
- 발행일
- 2013-08-15
- 유형
- Article
- 권
- 23
- 호
- 16
- 페이지
- 4713 ~ 4718
- 언어
- ENG
- 출판사
- Pergamon Press Ltd.
- 발행국가
- 영국
- 분량
- 6 페이지
- ISSN
- E 1464-3405
P 0960-894X