306964-85-2Relevant academic research and scientific papers
Computer-assisted design, synthesis and biological evaluation of novel pyrrolyl heteroaryl sulfones targeted at HIV-1 reverse transcriptase as non-nucleoside inhibitors
Silvestri, Romano,Artico, Marino,De Martino, Gabriella,Novellino, Ettore,Greco, Giovanni,Lavecchia, Antonio,Massa, Silvio,Loi, Anna Giulia,Doratiotto, Silvia,La Colla, Paolo
, p. 2305 - 2309 (2000)
Three pyrrolyl heteroaryl sulfones (ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate, ethyl 1-[(1H-benzimidazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate and ethyl 1-[(1H-benzotriazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate) were designed as novel HIV-1 reverse transcriptase non-nucleoside inhibitors using structure-based computational methods. Although these compounds were inactive in the cell-based assay, they inhibited the target enzyme with micromolar potency (IC50s=2μM, 3μM and 9μM, respectively). Copyright (C) 2000 Elsevier Science Ltd.
