Article
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
Journal of medicinal chemistry - 23 Aug 2007
Morningstar Marshall L, Roth Thomas, Farnsworth David W, Smith Marilyn Kroeger, Watson Karen, Buckheit Robert W, Das Kalyan, Zhang Wanyi, Arnold Eddy, Julias John G, Hughes Stephen H, Michejda Christopher J
Abstract excerpt
In an ongoing effort to develop novel and potent nonnucleoside HIV-1 reverse transcriptase (RT) inhibitors that are effective against the wild type (WT) virus and clinically observed mutants, 1,2-bis-substituted benzimidazoles were synthesized and tested. Optimization of the N1 and C2 positions of benzimidazole led to the development of 1-(2,6-difluorobenzyl)-2-(2,6-difluorophenyl)-4-methylbenzimidazole (1) (IC50...
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