Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Sweeney ZK, Dunn JP, Li Y, Heilek GM, Dunten PW, Elworthy TR, Han X, Harris SF, Hirschfeld DR, Hogg JH, Huber W, Kaiser AC, Kertesz DJ, Kim W, Mirzadegan T, Roepel MG, Saito YD, Silva TM, Swallow S, Tracy JL, Villasenor A, Vora H, Zhou AS, Klumpp K
Bioorganic & medicinal chemistry letters (2008), Volume 18, Page 4352
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Abstract:

A series of benzyl pyridazinones were evaluated as HIV-1 ...
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.

Polymerases:

HIV RT

Topics:

Structure and Structure/Function, Reverse Transcriptase

Status:

new topics/pols set partial results complete validated

Results:

Polymerase Reference Property Result Context
HIV RT Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase. Reverse Transcriptase Activity Yes
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Version:20241007

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