Synthesis And Evaluation Of Benzoxazinones As Hiv-1 Reverse Transcriptase Inhibitors. Analogs Of Efavirenz (Sustiva (Tm))

M Patel,Rj Mchugh,Bc Cordova,Rm Klabe,S Erickson-Viitanen,Gl Trainor,Ss Ko

Bioorganic & medicinal chemistry letters（1999）

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摘要

Two series of benzoxazinones differing in the aromatic substitution pattern were prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The 5-fluoro (5a-d) and 6-nitro (5e-h) substituted compounds displayed activity comparable or better than Efavirenz, the lead structure of the series. (C) 1999 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

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