2-Substitiuted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors

2-Substitiuted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors
2-Substitiuted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors

ㆍ 저자명: Shen. Gui-Nan,Choi. Jung-Ho,Gajulapati. Kondaji,Lee. Jee-Hyun,Kim. Young-Kook,Rho. Mun-Chal,Jung. Sang-Hun,Lee. Kyeong,Han. Sung
ㆍ 간행물명: Bulletin of the Korean Chemical Society
ㆍ 권/호정보: 2009년|30권 5호|pp.1088-1092 (5 pages)
ㆍ 발행정보: 대한화학회
ㆍ 파일정보: 정기간행물|ENG|
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ㆍ 주제분야: 기타

이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.

서지반출

기타언어초록

A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8- dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized and evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 5l and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with $IC_{50}$ value of 22.8 and 24.4 ${mu}M$, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 $sim$ 15 exhibited significant ACAT inhibitory activities.

키워드

Naphthoquinones Mast cells Acyl CoA: Cholestrol Acyl Transferase (ACAT)Structure-activity relationship

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