Design, Synthesis And Biological Evaluation Of Substituted 2-Amino-1,3-Thiazine Derivatives As Antituberculosis And Anti-Cancer Agents
SYNTHETIC COMMUNICATIONS(2019)
Abstract
A series of substituted 2-amino-1,3-thiazines were synthesized as amides (9a-9i), carbamates (9j-9m), sulfonamides (9n-9o) and urea derivatives (9p-9q) by treating the compound 7 with acid chlorides (8a-8i), chloroformates (8j-8m), sulfonyl chlorides (8n-8o) and isocyanates (8p-8q) respectively. The synthesized compounds (9a-9q) were screened for antituberculosis activity against Mycobacterium tuberculosis H(37)Rv ATCC 27294 and the results show that some of these derivatives possess good activity against Mycobacterium tuberculosis H(37)Rv ATCC 27294. A few also display promising cytotoxic activity against human breast cancer MCF-7 and human esophageal cancer EC-9706 cell lines. Regarding both biological profiles 9b, 9m and 9h are the most active for anti-cancer, anti-TB activity.[GRAPHICS].
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Key words
2-amino-1,3-thiazine,Mycobacterium tuberculosis H37Rv ATCC 27294,human breast cancer MCF-7,human esophageal cancer EC-9706,cytotoxic activity,antituberculosis agent,anticancer agent
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