Synthesis of isoniazid-1,2,3-triazole conjugates: Antitubercular, antimicrobial evaluation and molecular docking study

被引：21

作者：

Badar, Adinath D. ^{[1
]}

Sulakhe, Shubham M. ^{[1
]}

Muluk, Mahesh B. ^{[1
]}

Rehman, Naziya N. M. A. ^{[2
]}

Dixit, Prashant P. ^{[2
]}

Choudhari, Prafulla B. ^{[3
]}

Rekha, Estharla Madhu ^{[4
]}

Sriram, Dharmarajan ^{[4
]}

Haval, Kishan P. ^{[1
]}

机构：

[1] Dr Babasaheb Ambedkar Marathwada Univ SubCampus, Dept Chem, Osmanabad 413501, India

[2] Dr Babasaheb Ambedkar Marathwada Univ SubCampus, Dept Microbiol, Osmanabad, India

[3] Bharati Vidyapeeth Coll Pharm, Dept Pharmaceut Chem, Kolhapur, Maharashtra, India

[4] Birla Inst Technol & Sci Pilani, Dept Pharm, Hyderabad, India

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2020年 / 57卷 / 10期

关键词：

MYCOBACTERIUM-TUBERCULOSIS; 1,2,3-TRIAZOLE DERIVATIVES; BIOLOGICAL EVALUATION; IN-VITRO; DESIGN; BEARING; ANTIOXIDANT; ANTICANCER; THERAPY; AGENTS;

D O I：

10.1002/jhet.4072

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In the present study, a series of new isoniazid-1,2,3-triazole conjugates (5a-k) was synthesizedviaclick chemistry approach. The newly synthesized compounds were assessed for theirin vitroantitubercular and antimicrobial activities. The compound5ghas displayed potent antitubercular activity againstMycobacterium tuberculosisH37Rv (Mtb) with MIC value 1.56 mu g/mL. The active compounds were screened for their cytotoxicity profile by MTT assay against RAW 264.7 cell line. The four compounds have shown goodin vitroantimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study was accomplished to identify the probable mode of action of synthesized derivatives. These compounds have shown excellent binding affinity towardEnoyl-acp reductase(INHA) andDNA gyrase.

引用

页码：3544 / 3557

页数：14

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