P. Zhan, Hongbing Liu, Xinyong Liu
Sep 1, 2010
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1
Influential Citations
22
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Quality indicators
Journal
Medicinal Chemistry Research
Abstract
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 μM (CC50 of 169.24 ± 23.83μM) and 31.62 μM (CC50 > 309.06 μM), and resulting in selectivity index of 6 and >9, respectively. However, all newly synthesized derivatives were not active against HIV-2 replication.Graphical AbstractA series of novel N′-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio] acetohydrazides were synthesized and evaluated for their anti-HIV activities in MT-4 cell culture. Two compounds exhibited potent inhibitory activity specifically against HIV-1 replication.