Synthesis and evaluation of analogs of efavirenz (SUSTIVA TM) as HIV-1 reverse transcriptase inhibitors

…, BC Cordova, RM Klabe, S Erickson-Viitanen…

文献索引：Patel, Mona; Ko, Soo S.; McHugh Jr., Robert J.; Markwalder, Jay A.; Srivastava, Anurag S.; Cordova, Beverly C.; Klabe, Ronald M.; Erickson-Viitanen, Susan; Trainor, George L.; Seitz, Steven P. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 19 p. 2805 - 2810

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被引用次数: 69

摘要

Efavirenz (SUSTIVATM) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse transcriptase enzyme during Efavirenz therapy, we sought to develop an optimized second generation series. To that end, SAR of the substituents on the aromatic ring was undertaken and the results are summarized here. The 5, 6-difluoro (4f) and the 6-methoxy (4m) substituted ...