Synthesis and evaluation of antitubercular activity of glycosyl thio- and sulfonyl acetamide derivatives
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 H 37Rv. Amongst 32 compounds evaluated 3 compounds were effective in inhibitin...
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| Published in | Bioorganic & medicinal chemistry Vol. 18; no. 14; pp. 4002 - 4005 |
|---|---|
| Main Authors | , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford
Elsevier Ltd
15.07.2008
Elsevier |
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| 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 H
37Rv. 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. |
|---|---|
| AbstractList | 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 H(37)Rv. Amongst 32 compounds evaluated 3 compounds were effective in inhibiting mycobacterial growth at MIC of 6.25 microg/mL, 6 compounds at MIC of 3.125 microg/mL and 1 compound at MIC of 1.56 microg/mL. All active compounds were found nontoxic in Vero cell lines and mice bone marrow macrophages. 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 H sub(37)Rv. Amongst 32 compounds evaluated 3 compounds were effective in inhibiting mycobacterial growth at MIC of 6.25 mu g/mL, 6 compounds at MIC of 3.125 mu g/mL and 1 compound at MIC of 1.56 mu g/mL. All active compounds were found nontoxic in Vero cell lines and mice bone marrow macrophages. 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 H 37Rv. 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. |
| Author | Pandey, Shashi Tiwari, Pallavi Bhatnagar, Shalini Chaturvedi, Vinita Sinha, Sudhir Ghosh, Samir Gaikwad, Anil Misra, Anup Kumar |
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| Cites_doi | 10.1074/jbc.M004010200 10.1016/j.carres.2007.04.027 10.1021/ja00084a018 10.1080/07328300500256775 10.1046/j.1365-2958.1997.3361705.x 10.1021/jm000149l 10.1016/S1367-5931(97)80055-5 10.1093/labmed/9.3.47 10.1016/0022-1759(83)90303-4 10.1016/j.chembiol.2006.05.016 10.1146/annurev.bi.64.070195.000333 10.1074/jbc.M102272200 10.1016/j.bmcl.2007.01.068 10.1099/00221287-148-10-3059 10.1016/j.ejmech.2006.08.007 10.1021/ja9608555 10.1146/annurev.bi.42.070173.000321 10.1016/j.tetlet.2006.10.151 10.1016/S0008-6215(02)00541-4 10.1021/ja00199a081 10.1016/j.bmcl.2006.06.095 10.1016/S0005-2760(97)00051-9 10.1016/j.tetasy.2004.11.063 10.1517/14728222.6.1.21 10.1093/glycob/11.9.107R 10.1016/j.carres.2006.08.020 |
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| Keywords | Cell-wall biosynthesis Mycobacterial Glycosyl sulfonyl acetamide Antitubercular Glycosyl thioacetamide Sulfone Glycosyl thioacetamide,Glycosyl sulfonyl acetamide,Antitubercular,Mycobacterial,Cell-wall biosynthesis Biosynthesis In vitro Biological activity Cell wall Mycobacterium tuberculosis Mycobacteriales Thioglycoside Mycobacteriaceae Bacteria Carboxamide Actinomycetes Antituberculous agent Antibacterial agent Chemical synthesis |
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| SubjectTerms | Acetamides - chemistry Animals Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antitubercular Antitubercular Agents - chemical synthesis Antitubercular Agents - pharmacology Biological and medical sciences Bone Marrow Cells - cytology Cell-wall biosynthesis Cercopithecus aethiops Chemistry, Pharmaceutical - methods Drug Design Glycosyl sulfonyl acetamide Glycosyl thioacetamide Macrophages - metabolism Medical sciences Mice Microbial Sensitivity Tests Models, Chemical Mycobacterial Mycobacterium tuberculosis Mycobacterium tuberculosis - metabolism Pharmacology. Drug treatments Tuberculosis - drug therapy Vero Cells |
| Title | Synthesis and evaluation of antitubercular activity of glycosyl thio- and sulfonyl acetamide derivatives |
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