Attenuation of Mycobacterium species through direct and macrophage mediated pathway by unsymmetrical diaryl urea

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• 作者：Anand Babu Velappan^a ; Mamilla R. Charan Raja^b ; Dhrubajyoti Datta^c ; Yi Ting Tsai^d ; Iman Halloum^e ; Baojie Wan^f ; Laurent Kremer^e ; ^g ; Hugo Gramajo^d ; Scott G. Franzblau^f ; Santanu Kar Mahapatra^b ; ; Joy Debnath^a ; ^{joydebnath@scbt.sastra.edu} ; ^{joydebnathiitkgp@gmail.com}
• 关键词：Tuberculosis ; Diaryl urea ; Structure-activity relationship ; Antimycobacterial activity ; Cytotoxicity ; Mycolic acid ; Cytokines
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：825-841
• 全文大小：1428 K
• 卷排序：125

文摘

Different diaryl ureas are designed and synthesized. The antimycobacterial activity has been checked against M. smegmatis (mc2155) and M. tuberculosis (mc26030 and H37Rv strains). The EDG and EWG are found to have a preference for the ortho and meta positions of the first aromatic ring respectively. The effective molecules showed selective inhibitory activity on mycolic acid biosynthesis in 14C-radiolabelled assay. Effective molecules induced the upregulation of iNOS2, IFN-γ, IL-12 and downregulation of IL-10 to clear the infection.