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ID: ALA1134255

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain.

Authors: Cocuzza AJ, Chidester DR, Cordova BC, Jeffrey S, Parsons RL, Bacheler LT, Erickson-Viitanen S, Trainor GL, Ko SS.

Abstract: Two series of efavirenz analogues have been developed: one in which the cyclopropane ring has been replaced by small heterocycles and another in which the entire acetylenic side chain has been replaced by alkyloxy groups. Several members of both series show equivalent potency to efavirenz against both wild-type virus and the key K103N mutant.

CiteXplore: 11354371

DOI: 10.1016/s0960-894x(01)00192-5