Full metadata record

DC FieldValueLanguage
dc.contributor.author한서정-
dc.contributor.authorSuvarna H. Pagire-
dc.contributor.authorHaushabhau S. Pagire-
dc.contributor.authorGwi Bin Lee-
dc.contributor.authorHyun Jung Kwak-
dc.contributor.authorJi Young Kim-
dc.contributor.authorKi Young Kim-
dc.contributor.authorSang Dal Rhee-
dc.contributor.authorJeong Im Ryu-
dc.contributor.authorJin Sook Song-
dc.contributor.authorMyung Ae Bae-
dc.contributor.authorMi-jin Park-
dc.contributor.authorDooseop Kim-
dc.contributor.authorDuck Hyung Lee-
dc.contributor.authorJin Hee Ahn-
dc.date.accessioned2021-06-09T04:19:50Z-
dc.date.available2021-06-09T04:19:50Z-
dc.date.issued2015-08-
dc.identifier.citationVOL 101-735-
dc.identifier.issn0223-5234-
dc.identifier.other50504-
dc.identifier.urihttp://pubs.kist.re.kr/handle/201004/67373-
dc.description.abstractWe have developed a series of adamantane carboxylic acid derivatives exhibiting potent diacylglycerol acyltransferase 1 (DGAT1) inhibitory activities. Optimization of the series led to the discovery of E-adamantane carboxylic acid compound 43c, which showed excellent in vitro activity with an IC50 value of 5 nM against human and mouse DGAT1, also good druggability as well as microsomal stability and safety profiles such as hERG, CYP and cytotoxicity. Compound 43c significantly reduced plasma triglyceride levels in vivo (in rodents and zebrafish) and also showed bodyweight gain reduction and glucose area under curve (AUC) lowering efficacy in diet-induced obesity (DIO) mice.-
dc.publisherEuropean journal of medicinal chemistry-
dc.titleDiscovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes-
dc.typeArticle-
dc.relation.page716735-
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE