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


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.



Structure and Structure/Function, Reverse Transcriptase


new topics/pols set partial results complete validated


Polymerase Reference Property Result Context
HIV RT Sweeney ZK2008 Reverse Transcriptase Activity Yes

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