Different Heterocycles Functionalized s‐Triazine Analogues: Design,Synthesis and In Vitro Antimicrobial,Antituberculosis, and Anti‐HIV Assessment |
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Authors: | Paresh K. Patel Rahul V. Patel Dharmesh H. Mahajan Parimal A. Parikh Girish N. Mehta Christophe Pannecouque Erik De Clercq Kishor H. Chikhalia |
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Affiliation: | 1. Department of Applied Chemistry, Sardar Vallabhbhai National Institute of Technology (SVNIT), Surat, Gujarat, India;2. Department of Chemistry (CGBIBT), Uka Tarsadia University, Dist: Surat, Gujarat, India;3. Department of Chemical Engineering, Sardar Vallabhbhai National Institute of Technology (SVNIT), Surat, Gujarat, India;4. Rega Institute for Medical Research, KU Leuven, Leuven, Belgium;5. Department of Chemistry, School of Science, Gujarat University, Ahmedabad, Gujarat, India |
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Abstract: | Some new quinolone condensed s‐triazine derivatives endowed with different heterocycles and 4‐aminobenzonitrile moiety has been synthesized and examined for their bioactivities against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, and Shigella flexneri), two fungi (Aspergillus niger, Candida albicans) by using agar streak dilution method, and Mycobacterium tuberculosis H37Rv by using Lowenstein and Jensen MIC method. Upon preliminary biological screening, it was observed that the majority of the compounds were found to possess a significant broad spectrum antimicrobial (MICs: 6.25–25 µg/mL) and antitubercular (MIC: 12.5 µg/mL) potential. Hence, anti‐HIV activity against two types of HIV viral strains [HIV‐1 (IIIB) and HIV‐2 (ROD)] has been carried out using the MTT assay. From this bioassay, we have identified some potent inhibitors acting as anti‐HIV‐1 agents (IC50: 4.45 µg/mL) with promising therapeutic index of 16 for analogue 7 h. The structural assignments of the new products were carried out on the basis of IR, 1H NMR, 13C NMR spectroscopy, and elemental analysis. |
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