Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl)phenothiazine-[1,2,3]triazole hybrids

被引：50

作者：

Addla, Dinesh ^{[1
]}

Jallapally, Anvesh ^{[1
]}

Gurram, Divya ^{[1
]}

Yogeeswari, Perumal ^{[2
]}

Sriram, Dharmarajan ^{[2
]}

Kantevari, Srinivas ^{[1
,3
]}

机构：

[1] CSIR, Indian Inst Chem Technol, CPC Div, Organ Chem Div 2, Hyderabad 500007, Andhra Pradesh, India

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

[3] CSIR, Indian Inst Chem Technol, Acad Sci & Innovat Res, Hyderabad 500007, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

关键词：

Phenothiazine; Triazoles; Molecular hybridization; Antimycobacterial activity; Mycobacterium tuberculosis; MULTIDRUG-RESISTANT TUBERCULOSIS; MOLECULAR HYBRIDIZATION; PHENOTHIAZINES; DRUGS;

D O I：

10.1016/j.bmcl.2013.11.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Molecular hybridization is an emerging structural modification tool to design molecules with better pharmacophoric properties. A series of novel 2-(trifluoromethyl)phenothiazine-1,2,3-triazoles 5a-v designed by hybridizing two antitubercular drugs trifluoperazine and I-A09 in a single molecular architecture, were synthesized in very good yields using click chemistry. Among the all '22' compounds screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (Mtb), three analogs 5c, 5l and 5o were found to be most potent (MIC: 6.25 mu g/mL) antitubercular agents with good selectivity index. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：233 / 236

页数：4

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