Nitroimidazoles Part 7. Synthesis and Anti-HIV Activity of New 4-Nitroimidazole Derivatives

作者:Al Masoudi Najim A*; Pfleiderer Wolfgang; Pannecouque Christophe
来源:Zeitschrift fur Naturforschung Section B-A Journal of Chemical Sciences, 2012, 67(8): 835-842.
DOI:10.5560/ZNB.2012-0122

摘要

Reverse transeriptase enzyme (RT) is an attractive target for the development of new drugs useful in AIDS therapy and HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs), and offers the possibility of generating structures of increased potency. On this basis, a series of 4-oxo-3-pheny1-2-(phenylimino)thiazolidin-5-ylidene, 3-hydroxypropyl, 3-azidopropyl, and 3-aminopropyl derivatives of 1-benzyl-2-ethyl-4-nitroimidazoles 6-8, as well as the substituted 1,2,3-triazolo analogs 12-14, the diazepam 15 and earboxamide derivatives 16 and 17 were synthesized. All compounds have been evaluated for their anti-HIV activity.