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Synthesis and evaluation of antitubercular activity of glycosyl thio- and sulfonyl acetamide derivatives
Authors:Ghosh Samir  Tiwari Pallavi  Pandey Shashi  Misra Anup Kumar  Chaturvedi Vinita  Gaikwad Anil  Bhatnagar Shalini  Sinha Sudhir
Institution:aMedicinal and Process Chemistry Division, Central Drug Research Institute, Chattar Manzil Palace, Lucknow 226001, UP, India;bDrug Target Discovery and Development Division, Central Drug Research Institute, Lucknow 226001, India
Abstract:A series of glycosyl thioacetamide and glycosyl sulfonyl acetamide derivatives have been prepared following a convenient reaction protocol and evaluated for their antitubercular activity against Mycobacterium tuberculosis H37Rv. Amongst 32 compounds evaluated 3 compounds were effective in inhibiting mycobacterial growth at MIC of 6.25 μg/mL, 6 compounds at MIC of 3.125 μg/mL and 1 compound at MIC of 1.56 μg/mL. All active compounds were found nontoxic in Vero cell lines and mice bone marrow macrophages.
Keywords:Glycosyl thioacetamide  Glycosyl sulfonyl acetamide  Antitubercular  Mycobacterial  Cell-wall biosynthesis
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