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Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitorsopen access
- Authors
- Hong, Dong Jin; Jung, Seung Hyun; Kim, Jisook; Jung, Danbee; Ahn, Young Gil; Suh, Kwee Hyun; Min, Kyung Hoon
- Issue Date
- 1-Jan-2020
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- DGAT-1; obesity; small molecules; thienopyrimidine; type 2 diabetes
- Citation
- JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.35, no.1, pp 227 - 234
- Pages
- 8
- Journal Title
- JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Volume
- 35
- Number
- 1
- Start Page
- 227
- End Page
- 234
- ISSN
- 1475-6366
1475-6374
- Abstract
- A novel series of thieno[3,2-d]pyrimidine derivatives were synthesised and their inhibitory effects against diacylglycerol acyltransferase 1 (DGAT-1) were assessed. cis-Isomer 17a showed potent and selective inhibitory activity against DGAT-1 in SF9 cells. In addition, 17a had an acceptable pharmacokinetic profile and accumulated mainly in the small intestine and liver. Oral administration of 17a led to a significant reduction in plasma triacylglycerol level during an oral lipid tolerance test (OLTT) in murine and canine models. Taken together, 17a is a high-quality candidate that deserves further investigation.
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