Design and synthesis of N1-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

被引：49

作者：

Monforte, Anna-Maria ^{[1
]}

Ferro, Stefania ^{[1
]}

De Luca, Laura ^{[1
]}

Lo Surdo, Giuseppa ^{[1
]}

Morreale, Francesca ^{[1
]}

Pannecouque, Christophe ^{[2
]}

Balzarini, Jan ^{[2
]}

Chimirri, Alba ^{[1
]}

机构：

[1] Univ Messina, Dipartimento Sci Farmaco & Prod Salute, I-98168 Messina, Italy

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 04期

关键词：

HIV-1 reverse transcriptase; NNRTIs; N-1-Aryl-benzimidazoles; 2-substituted; Synthesis; IMMUNODEFICIENCY-VIRUS TYPE-1; WILD-TYPE; POTENT; DISCOVERY; ANALOGS; UPDATE;

D O I：

10.1016/j.bmc.2013.12.045

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel N-1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：1459 / 1467

页数：9

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