Medicinal Chemistry Research vol:19 issue:7 pages:652-663
A series of novel N'-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio]acetohydrazides was synthesized and evaluated, as nonnucleoside reverse transcriptase inhibitors (NNRTIs), for their in vitro HIV-1 and HIV-2 activity using the IIIB strain and ROD strain, respectively. The activity was monitored by the inhibition of the virus-induced cytopathic effect in the human T-lymphocyte (MT-4) cells. All of the new compounds were structurally confirmed by spectral analyses. Compounds 5q and 5r showed EC50 of 29.62 mu M (CC50 of 169.24 +/- 23.83 mu M) and 31.62 mu M (CC50 >309.06 mu M), and resulting in selectivity index of 6 and >9, respectively. However, all newly synthesized derivatives were not active against HIV-2 replication.