| Literature DB >> 18632268 |
Zachary K Sweeney1, James P Dunn, Yu Li, Gabrielle Heilek, Pete Dunten, Todd R Elworthy, Xiaochun Han, Seth F Harris, Donald R Hirschfeld, J Heather Hogg, Walter Huber, Ann C Kaiser, Denis J Kertesz, Woongki Kim, Taraneh Mirzadegan, Michael G Roepel, Y David Saito, Tania M P C Silva, Steven Swallow, Jahari L Tracy, Armando Villasenor, Harit Vora, Amy S Zhou, Klaus Klumpp.
Abstract
A series of benzyl pyridazinones were evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Several members of this series showed good activity against the wild-type virus and NNRTI-resistant viruses. The binding of inhibitor 5a to HIV-RT was analyzed by surface plasmon resonance spectroscopy. Pharmacokinetic studies of 5a in rat and dog demonstrated that this compound has good oral bioavailability in animal species. The crystal structure of a complex between HIV-RT and inhibitor 4c is also described.Entities:
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Year: 2008 PMID： 18632268 DOI： 10.1016/j.bmcl.2008.06.072
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823