Synthesis and molecular modeling studies of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones as novel anti-filarial agents

被引：24

作者：

Chhajed, Santosh S. ^{[1
]}

Manisha, Puranik ^{[2
]}

Bastikar, Virupaksha A. ^{[3
]}

Animeshchandra, Haldar ^{[4
]}

Ingle, V. N. ^{[4
]}

Upasani, Chandrashekhar D. ^{[5
]}

Wazalwar, Sachin S. ^{[6
]}

机构：

[1] SMBT Coll Pharm, Dept Pharmaceut Chem, Dhamangaon, MS, India

[2] Inst Pharmaceut Educ & Res, Wardha, MS, India

[3] Dr DY Patil Inst Biotechnol & Bioinformat, Belapur, Navi Mumbai, India

[4] RTM Nagpur Univ, Dept Chem, Nagpur, MS, India

[5] SSDJ Coll Pharm, Chandwad, MS, India

[6] Rajiv Gandhi Coll Engn, Chandrapur, MS, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期

关键词：

Synthesis; Azetidin-2-ones; In vitro anti-filarial; Molecular docking; MDS; ANTIFILARIAL PROFILE; TRANSFERASE; GLUTATHIONE;

D O I：

10.1016/j.bmcl.2010.04.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (Va-f) on a structural basis, automated docking studies were carried out with Molecular Design Suite (MDS v 3.5) into the active site of glutathione-S-transferase (GST) enzyme; scoring functions of these compounds at the active site of the GST enzyme were used for correlation with observed activity. Compounds V-e and V-f have shown good affinity for receptor GST, as well as in vitro anti-filarial potency. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3640 / 3644

页数：5

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