| Literature DB >> 20359891 |
Tomoharu Tsukada1, Kazuhiko Tamaki, Jun Tanaka, Toshiyuki Takagi, Taishi Yoshida, Akira Okuno, Takeshi Shiiki, Mizuki Takahashi, Takahide Nishi.
Abstract
For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug 4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug 20, which strongly inhibited glucose production in monkey hepatocytes and also showed weak CYP3A4 inhibitory potency. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20359891 DOI： 10.1016/j.bmcl.2010.03.017
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823