Ontology highlight
ABSTRACT:
SUBMITTER: Morningstar ML
PROVIDER: S-EPMC3057568 | biostudies-literature | 2007 Aug
REPOSITORIES: biostudies-literature
Morningstar Marshall L ML Roth Thomas T Farnsworth David W DW Smith Marilyn Kroeger MK Watson Karen K Buckheit Robert W RW Das Kalyan K Zhang Wanyi W Arnold Eddy E Julias John G JG Hughes Stephen H SH Michejda Christopher J CJ
Journal of medicinal chemistry 20070731 17
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 = 0.2 microM, EC50 = 0.44 microM, and TC50 >/= 100 against WT). This paper describe ...[more]