Synthesis and antimycobacterial activities of some new thiazolylhydrazone derivatives |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey;2. Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science–Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India;1. Faculty of Mechanical Engineering and Mechatronics, Institute of Physics, West Pomeranian University of Technology, Al. Piastów 17, 70-310 Szczecin, Poland;2. Faculty of Engineering, Kyoto Sangyo University, Kamigamo, Kyoto 603-8555, Japan;3. Institute of Advanced Materials, Nanjing University of Technology, Nanjing 210009, China;4. Institute of Physics, Polish Academy of Sciences, Al. Lotników 32/46, 00-908 Warsaw, Poland;1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 2A Nanwei Road, Xuanwu District, Beijing 100050, PR China;2. Department of Microbiology and Immunology, Weill Cornell Medical College, New York, NY 10065, USA;3. Tsinghua-Peking Center for Life Sciences and School of Medicine, Tsinghua University, Haidian Dist., Beijing 100084, PR China;4. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Haidian Dist., Beijing 100084, PR China;5. Division of Infectious Diseases, Department of Medicine, Weill Cornell Medical College, New York, NY 10065, USA |
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| Abstract: | This Letter reports the synthesis and evaluation of some thiazolylhydrazone derivatives for their in vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv. The cytotoxic activities of all compounds were also evaluated. The compounds exhibited promising antimycobacterial activity with MICs of 1.03–72.46 μM and weak cytotoxicity (8.9–36.8% at 50 μg/mL). Among them, 1-(4-(1H-1,2,4-triazol-1-yl)benzylidene)-2-(4-(4-nitrophenyl)thiazol-2-yl)hydrazine 10 was found to be the most active compound (MIC of 1.03 μM) with a good safety profile (16.4% at 50 μg/mL). Molecular modeling studies were done to have an idea for the mechanism of the action of the target compounds. According the docking results it can be claimed that these compounds may bind most likely to TMPK than InhA or CYP121. |
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| Keywords: | Thiazolylhydrazone Antimycobacterial activity Cytotoxicity Docking |
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