Ciprofloxacin-1,2,3-triazole-isatin hybrids tethered via amide: Design,synthesis, and in vitro anti-mycobacterial activity evaluation |
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| Institution: | 1. Xuzhou Women & Children’s Healthcare Hospital, Xuzhou 221009, Jiangsu Province, PR China;2. Xuzhou Central Hospital, Department of Neurosurgery, Second Division, Xuzhou 221009, Jiangsu Province, PR China;1. State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People''s Republic of China;2. Structural Biology Laboratory, Tsinghua University, Beijing 100084, People''s Republic of China;1. Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi, Viet Nam;2. Lab of Profession Chemistry, Institute of Biochemical Technology and Profession Documents, General Department 4 (Ministry of Public Security), 80 Tran Quoc Hoan, Cau Giay, Ha Noi, Viet Nam;3. Institute for Chemistry and Materials, Military Institute of Science and Technology, 17 Hoang Sam, Cau Giay, Ha Noi, Viet Nam;4. Viet Tri University of Industry, Tien Kien, Lam Thao, Phu Tho, Viet Nam;5. Thai Nguyen College of Education, Quang Trung, Thinh Dan, Thai Nguyen, Viet Nam;6. Faculty of Chemistry, Thai Nguyen University of Education, 20 Luong Ngoc Quyen, Thai Nguyen, Viet Nam;1. Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India;2. Department of Medicine, University of California, San Francisco, CA, USA;1. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;2. Pharmacology and Toxicology Division, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;1. Faculty of Science and Technology, Quest International University Perak, Ipoh, 30250, Perak, Malaysia;2. Department of Paediatrics, Zhuji Affiliated Hospital of Shaoxing University, Shaoxing, China |
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| Abstract: | The purpose of this study was to prepare various novel amide tethered ciprofloxacin-1,2,3-triazole-isatin hybrids 7a-l, and evaluate their in vitro anti-mycobacterial activity as well as cytotoxicity in VERO cells. The synthesized hybrids showed considerable in vitro activity against both MTB H37Rv and MDR-MTB with MIC of 0.12 to 32 μg/mL, and acceptable cytotoxicity in VERO cells (CC50: 8.0–>128.0 μg/mL). In particular, the most active hybrid 7a (MICMTB H37Rv: 0.5 μg/mL and MICMDR-MTB: 0.12 μg/mL) had the activity in the same level with the first-line anti-tubercular agents isoniazid (MIC: 0.12 μg/mL) and rifampicin (MIC: 0.25 μg/mL), and it was 2-fold more active than the parent ciprofloxacin (MIC: 1.0 μg/mL) against MTB H37Rv, and ≥16 folds more potent than ciprofloxacin (MIC: 2.0 μg/mL), isoniazid (MIC: >64 μg/mL) and rifampicin (MIC: >64 μg/mL) against MDR-MTB. Moreover, hybrid 7a (CC50: 16.0 μg/mL) also displayed considerable cytotoxicity towards VERO cells. Thus, hybrid 7a could act as a platform for further investigations. |
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| Keywords: | Ciprofloxacin Isatin 1 2 3-triazole Anti-mycobacterial Anti-tubercular Drug-resistant |
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