상세 보기
Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives
- Han, Seo-Jung;
- Lee, Gwi Bin;
- Kwak, Hyun Jung;
- Pagire, Suvarna H.;
- Kim, Ji Young;
- ... Lee, Duck Hyung;
- 외 12명
Citations
WEB OF SCIENCE
1Citations
SCOPUS
1초록
We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferase-1 (DGAT)-1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGAT-1, selectivity toward DGAT-2, and liver microsomal stability. Compound 6b exhibited no CYP inhibition, hERG binding, or cell cytotoxicity. Additionally, compound 6b reduced the level of plasma triglyceride after oral administration in mice.
키워드
Diacylglycerol acyltransferase-1; Triglycerides; 3-Azabicyclo[3.1.0]hexane; Oral lipid tolerance test; DGAT1 INHIBITORS; TRIGLYCERIDE SYNTHESIS; BIOLOGICAL EVALUATION; KEY ENZYME; DISCOVERY; OBESITY; MICE; ISOXAZOLE; ANALOGS; POTENT
- 제목
- Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives
- 저자
- Han, Seo-Jung; Lee, Gwi Bin; Kwak, Hyun Jung; Pagire, Suvarna H.; Kim, Ji Young; Pagire, Haushabhau S.; Park, Sung Bum; Chae, Chong Hak; Lee, Joo Yun; Kim, Ki Young; Rhee, Sang Dal; Kim, Hee Youn; Shin, Sun Hye; Bae, Myung Ae; Park, Mi-jin; Kim, Dooseop; Lee, Duck Hyung; Ahn, Jin Hee
- 발행일
- 2015-06
- 유형
- Article
- 권
- 36
- 호
- 6
- 페이지
- 1586 ~ 1593
- 언어
- ENG
- 출판사
- 대한화학회
- 발행국가
- 대한민국
- 분량
- 8 페이지
- ISSN
- E 1229-5949
P 0253-2964