Synthesis and anti-HIV-1 activity of 4, 5, 6, 7-tetrahydro-5-methylimidazo [4, 5, 1-jk][1, 4] benzodiazepin-2 (1H)-one (TIBO) derivatives

…, R Pauwels, CL Fedde, M Miranda…

Index: Kukla, Michael J.; Breslin, Henry J.; Pauwels, Rudi; Fedde, Cynthia L.; Miranda, Milton; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 746 - 751

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Citation Number: 123

Abstract

A series of 6-substituted 4, 5, 6, 7-tetrahydro-5-methylimidazo [4, 5, l-jk][1, 4] benzodiazepin- 2 (1H)-ones (9) have been synthesized and tested for their ability to inhibit the replication of the HIV-1 virus in MT-4 cells. Two synthetic methods are described, one of which allows the synthesis of single enantiomen of the final products. A structur~ ctivity study was done within the series of compounds to determine the optimum group for the 6-position substitution ...