Novel cyclopropyl-indole derivatives as HIV non-nucleoside reverse transcriptase inhibitors

Hassam M. ; Basson A.E. ; Liotta D.C. ; Morris L. ; Van Otterlo W.A.L. ; Pelly S.C. (2012)


The HIV pandemic represents one of the most serious diseases to face mankind in both a social and economic context, with many developing nations being the worst afflicted. Due to ongoing resistance issues associated with the disease, the design and synthesis of anti-HIV agents presents a constant challenge for medicinal chemists. Utilizing molecular modeling, we have designed a series of novel cyclopropyl indole derivatives as HIV non-nucleoside reverse transcriptase inhibitors and carried out their preparation. These compounds facilitate a double hydrogen bonding interaction to Lys101 and efficiently occupy the hydrophobic pockets in the regions of Tyr181/188 and Val179. Several of these compounds inhibited HIV replication as effectively as nevirapine when tested in a phenotypic assay. © 2012 American Chemical Society.

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