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

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

Index: 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

Full Text: HTML

Citation Number: 69

Abstract

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 ...