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Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2008
Zachary K Sweeney, and
James P Dunn, and
Yu Li, and
Gabrielle Heilek, and
Pete Dunten, and
Todd R Elworthy, and
Xiaochun Han, and
Seth F Harris, and
Donald R Hirschfeld, and
J Heather Hogg, and
Walter Huber, and
Ann C Kaiser, and
Denis J Kertesz, and
Woongki Kim, and
Taraneh Mirzadegan, and
Michael G Roepel, and
Y David Saito, and
Tania M P C Silva, and
Steven Swallow, and
Jahari L Tracy, and
Armando Villasenor, and
Harit Vora, and
Amy S Zhou, and
Klaus Klumpp
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. zachary.sweeney@roche.com
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.
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