Synthesis and bioevaluation of glycosyl ureas as alpha-glucosidase inhibitors and their effect on mycobacterium |
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| Authors: | Tewari Neetu Tiwari V K Mishra R C Tripathi R P Srivastava A K Ahmad R Srivastava R Srivastava B S |
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| Affiliation: | Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow-226001, India. |
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| Abstract: | Glycosyl amino esters (2-13) on reaction with different isocyanates resulted in quantitative conversion to glycosyl ureas (14--32). Few of the selected ureas (15-20, 22-28, 30 and 32) on cyclative amidation with DBU/TBAB/4 A MS gave respective dihydropyrimidinones in fair to good yields (33-47). The compounds were screened for alpha-glucosidase inhibitory activity and two (19 and 23) of them showed strong inhibition against rat intestinal alpha-glucosidase. The compounds were also screened against Mycobacterium aurum, however, only one (19) of them exhibited marginal antitubercular activity. |
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