期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 14, 页码 4227-4237出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.05.062
关键词
Groebke reaction; Imidazo[1,2-a]pyridine; NNRTI; Reverse transcriptase; Antiretroviral; HIV
During random screening of a small in-house library of compounds, certain substituted imidazo[1,2-a]pyridines were found to be weak allosteric inhibitors of HIV-1 reverse transcriptase (RT). A library of these compounds was prepared using the Groebke reaction and a subset of compounds prepared from 2-chlorobenzaldehyde, cyclohexyl isocyanide and a 6-substituted 2-aminopyridine showed good inhibitory activity in enzymatic (RT) and HIV anti-infectivity MAGI whole cell assays. The compound showing the best anti-HIV-1 IIIB whole cell activity (MAGI IC(50) = 0.18 mu M, IC(90) = 1.06 mu M), along with a good selectivity index (>800), was 2-(2-chlorophenyl)-3-(cyclohexylamino) imidazo[1,2-a]pyridine-5-carbonitrile 38. (C) 2011 Elsevier Ltd. All rights reserved.
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