SrasV1, Main, Exploration, bibRecord, 002C92

Synthesis and anti-HIV activity evaluation of novel N ′-arylidene-2-[1-(naphthalen-1-yl)-1 H -tetrazol-5-ylthio]acetohydrazides

Identifieur interne : 002C92 ( Main/Exploration ); précédent : 002C91; suivant : 002C93

Synthesis and anti-HIV activity evaluation of novel N ′-arylidene-2-[1-(naphthalen-1-yl)-1 H -tetrazol-5-ylthio]acetohydrazides

Auteurs : Peng Zhan [République populaire de Chine] ; Hongbing Liu [République populaire de Chine] ; Xinyong Liu [République populaire de Chine] ; Yan Wang [République populaire de Chine] ; Christophe Pannecouque [Belgique] ; Myriam Witvrouw [Belgique] ; Erik De Clercq [Belgique]

Source :

Medicinal Chemistry Research [ 1054-2523 ] ; 2010-09-01.

RBID : ISTEX:55A5BEFD982BE6AC58F668CB35500CF60D434AC7

Descripteurs français

Wicri :
- topic : Sida.

English descriptors

KwdEn :
- AIDS, Acetohydrazides, Antiviral activity, HIV-1, NNRTIs, Tetrazole.

Abstract

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 Abstract: A 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.

Url:

https://api.istex.fr/ark:/67375/VQC-VLS8LPLD-S/fulltext.pdf

DOI: 10.1007/s00044-009-9220-x

Affiliations:

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Le document en format XML

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<front><div type="abstract" xml:lang="en">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 Abstract: A 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.</div>
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Synthesis and anti-HIV activity evaluation of novel N ′-arylidene-2-[1-(naphthalen-1-yl)-1 H -tetrazol-5-ylthio]acetohydrazides

Synthesis and anti-HIV activity evaluation of novel N ′-arylidene-2-[1-(naphthalen-1-yl)-1 H -tetrazol-5-ylthio]acetohydrazides

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri