Title of article
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase
Author/Authors
Zachary K. Sweeney، نويسنده , , James P. Dunn، نويسنده , , Yu Li، نويسنده , , Gabrielle Heilek، نويسنده , , Pete Dunten، نويسنده , , Todd R. Elworthy، نويسنده , , Xiaochun Han، نويسنده , , Seth F. Harris، نويسنده , , Donald R. Hirschfeld، نويسنده , , J. Heather Hogg، نويسنده , , Walter Huber، نويسنده , , Ann C. Kaiser، نويسنده , , Denis J. Kertesz، نويسنده , , Woongki Kim، نويسنده , , Taraneh Mirzadegan، نويسنده , , Michael G. Roepel، نويسنده , , Y. David Saito، نويسنده , , Tania M.P.C. Silva، نويسنده , , Steven Swallow، نويسنده , , Jahari L. Tracy، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
3
From page
4352
To page
4354
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.
Keywords
HIV , Human Immunodeficiency Virus , Non-nucleoside , reverse transcriptase , NNRTI
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799781
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