Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives

被引：69

作者：

Narang, Rakesh ^{[2
]}

Narasimhan, Balasubramanian ^{[1
]}

Sharma, Sunil ^{[2
]}

Sriram, Dharmarajan ^{[3
]}

Yogeeswari, Perumal ^{[3
]}

De Clercq, Erik ^{[4
]}

Pannecouque, Christophe ^{[4
]}

Balzarini, Jan ^{[4
]}

机构：

[1] Maharshi Dayanand Univ, Fac Pharmaceut Sci, Rohtak 124001, Haryana, India

[2] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India

[3] Birla Inst Technol & Sci, Pharm Grp, Med Chem Res Lab, Hyderabad 500078, Andhra Pradesh, India

[4] Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 08期

关键词：

Hydrazides; Antimycobacterial; Antiviral; Antimicrobial; QSAR; QUANTITATIVE STRUCTURE; ANTIBACTERIAL ACTIVITY; UNIFIED QSAR; PREDICTION; CHEMISTRY; NETWORKS; ANTAGONISTS; HYDRAZONES; ANALOGS; 3D-QSAR;

D O I：

10.1007/s00044-011-9664-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of nicotinic acid benzylidene hydrazide derivatives (1-18) was synthesized and tested in vitro for biological evaluations. The antimycobacterial activity results indicated that the presence of electron-withdrawing halogen groups at para position of the phenyl ring improved their activity. The results of antiviral evaluation depicted that none of the synthesized derivatives inhibited the replication of viruses at subtoxic concentration. Further, the antimicrobial screening results indicated that compounds having OCH3 and NO2 substituents were the most active ones. QSAR investigations revealed that multi-target QSAR models were effective in describing the antimicrobial activity.

引用

页码：1557 / 1576

页数：20

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