Novel isoniazid embedded triazole derivatives: Synthesis,antitubercular and antimicrobial activity evaluation |
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| Affiliation: | 1. Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University SubCampus, Osmanabad 413501, MS, India;2. Department of Pharmaceutical Chemistry, School of Pharmacy, Vishwakarma University, Pune 411048, MS, India;3. Department of Microbiology, Dr. Babasaheb Ambedkar Marathwada University SubCampus, Osmanabad 413501, MS, India;4. Department of Pharmacy, Birla Institute of Technology and Science-Pilani, Hyderabad Campus, Jawahar Nagar, Shameerpet Mandal, R. R. District, Hyderabad 500078, India;1. Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India;2. Institut de Recherche en Infectiologie (IRIM) de Montpellier, CNRS, UMR 9004 Université de Montpellier, France;3. INSERM, IRIM, 34293 Montpellier, France;4. School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa;1. Instituto de Química Rosario, UNR, CONICET, Suipacha 531, S2002LRK, Rosario, Argentina;2. Laboratorio de Microbiología Molecular, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2002KTR, Rosario, Argentina;3. IQUIBICEN-CONICET, Ciudad Universitaria, Pabellón 2, C1428EHA, Ciudad de Buenos Aires, Argentina;4. Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, C1428EHA, Ciudad de Buenos Aires, Argentina;5. Consejo de Investigaciones Científicas, Universidad Nacional de Rosario, Argentina;6. Departamento de Química Orgánica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, S2002LRK, Rosario, Argentina;1. Laboratory of Organic Synthesis and Biopharmaceuticals, Institute of Chemistry, Chisinau, 3 str. Academiei, Moldova;2. Scientific Center for Drug Research, “Nicolae Testemitanu” State University of Medicine and Pharmacy, Chisinau, Moldova;3. Department of Pharmacy School of Health, Department of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece;4. Department of Plant Physiology, Institute for Biological Research “Siniša Stanković” – National Institute of Republic of Serbia,University of Belgrade, Bulevar despota Stefana 142, 11000, Belgrade;5. Laboratory of Physical Methods of Solid State Investigation ″Tadeusz Malinowski, Institute of Applied Physics, Chisinau, 5 str. Academiei, Moldova;1. Department of Chemistry, School of Sciences, Gujarat University, Ahmedabad, India;2. Department of Life Sciences, School of Sciences, Gujarat University, Ahmedabad, India;3. Department of Bioinformatics, Applied Botany Centre (ABC), School of Sciences, Gujarat University, Ahmedabad, 380009, Gujarat, India;1. Department of Studies in Chemistry, Bangalore University, Bengaluru, 560 059, Karnataka, India;2. P.G. Department and Research Studies in Chemistry, Government Science College, Bengaluru, 560 001, Karnataka, India;3. P.G. Department of Chemistry, Vijaya College, R.V. Road, Bengaluru, Karnataka, 560 004, India;4. Department of Chemistry, Guru Nanak First Grade College, Bidar, 585 403, Karnataka, India |
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| Abstract: | In the present study, a series of new isoniazid embedded triazole derivatives have been synthesized. These compounds were evaluated for their in vitro antitubercular and antimicrobial activities. Among the screened compounds, six have exhibited potent antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MIC value 0.78 μg/mL, whereas, three compounds have displayed activity with MIC value ranging from 1.56 to 3.125 μg/mL. The cytotoxicity of the active compounds was studied against RAW 264.7 cell line by MTT assay and no toxicity was observed even at 25 μg/mL concentration. The five compounds have displayed good antimicrobial activities. Molecular docking have been performed against mycobacterial InhA enzyme to gain an insight into the plausible mechanism of action which could pave the way for our endeavor to identify potent antitubercular candidates. We believe that further optimization of these molecules may lead to potent antitubercular agents. |
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| Keywords: | Isoniazid 1, 2, 3-Triazole Antitubercular activity Antimicrobial activity Cytotoxicity Molecular docking Click chemistry |
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