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

Adinath D. Badar; Shubham M. Sulakhe; Mahesh B. Muluk; Naziya N. M. A. Rehman; Prashant P. Dixit; Prafulla B. Choudhari; Estharla Madhu Rekha; Dharmarajan Sriram; Kishan P. Haval

doi:10.1002/jhet.4072

journal article Aug 05, 2020

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

Adinath D. Badar Shubham M. Sulakhe Mahesh B. Muluk Naziya N. M. A. Rehman Prashant P. Dixit Prafulla B. Choudhari Estharla Madhu Rekha Dharmarajan Sriram Kishan P. Haval

Journal of Heterocyclic Chemistry Vol. 57 No. 10 pp. 3544-3557 · Wiley

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Abstract

AbstractIn the present study, a series of new isoniazid‐1,2,3‐triazole conjugates (5a‐k) was synthesized via click chemistry approach. The newly synthesized compounds were assessed for their in vitro antitubercular and antimicrobial activities. The compound 5g has displayed potent antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb) with MIC value 1.56 μg/mL. The active compounds were screened for their cytotoxicity profile by MTT assay against RAW 264.7 cell line. The four compounds have shown good in vitro antimicrobial 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 toward Enoyl‐acp reductase (INHA) and DNA gyrase.

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Details

Published: Aug 05, 2020
Vol/Issue: 57(10)
Pages: 3544-3557
License: View

Authors

A

Adinath D. Badar

Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

S

Shubham M. Sulakhe

Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

M

Mahesh B. Muluk

Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

N

Naziya N. M. A. Rehman

Department of Microbiology Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

P

Prashant P. Dixit

Department of Microbiology Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

P

Prafulla B. Choudhari

Department of Pharmaceutical Chemistry Bharati Vidyapeeth College of Pharmacy Kolhapur India

E

Estharla Madhu Rekha

Department of Pharmacy Birla Institute of Technology and Science‐Pilani Hyderabad India

D

Dharmarajan Sriram

Department of Pharmacy Birla Institute of Technology and Science‐Pilani Hyderabad India

K

Kishan P. Haval

Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University SubCampus Osmanabad India

Cite This Article

Adinath D. Badar, Shubham M. Sulakhe, Mahesh B. Muluk, et al. (2020). Synthesis of isoniazid‐1,2,3‐triazole conjugates: Antitubercular, antimicrobial evaluation and molecular docking study. Journal of Heterocyclic Chemistry, 57(10), 3544-3557. https://doi.org/10.1002/jhet.4072

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

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