Synthesis and anti-HIV activity of novel macrocyclic benzamides with a disulphide bridge

摘要

A series of macrocyclic dilactanis containing a disuiphide bridge has been synthesized by the condensation of 2,2’-dithiodibenzoyl chloride with diamines. These compounds have been evaluated for their ability to inhibit reverse transcriptase (RT) of the human immuno deficiency virus HIV-l (III_B) and H1V-2 (ROD) in acutely infected MT-4 cells. The anti-I-IIV activity of these compounds depends on the ring size and also on the dianiino counterpart. The dilactams with 12-membered rings 1 and 5 were found to be the most potent. The active analogues 1 and 5 inhibit the replication of HIV-1 (III_B) and HIV-2 (ROD) with an BC_(50) between 1.2 to 4.4 #mu#g/mL. The dilactam 7 shows comparable activity in C 8166 cells.