Synthesis and evaluation of small libraries of triazolylmethoxy chalcones, flavanones and 2-aminopyrimidines as inhibitors of mycobacterial FAS-II and PknG

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• 作者：Namrata An ; Priyanka Singh ; Anindra Sharma ; Sameer Tiwari ; V ; ana Singh ; Diwakar K. Singh ; Kishore K. Srivastava ; B.N. Singh ; Rama Pati Tripathi
• 关键词：Triazolylmethoxy chalcones ; 2-Aminopyrimidines ; Triazolylmethoxy flavanones ; Mycobacterium tuberculosis ; FAS-II ; PknG
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 出版时间：1 September, 2012
• 年：2012
• 卷：20
• 期：17
• 页码：5150-5163
• 全文大小：917 K

文摘

A synthetic strategy to access small libraries of triazolylmethoxy chalcones 4{1-20}, triazolylmethoxy flavanones 5{1-10} and triazolylmethoxy aminopyrimidines 6{1-17} from a common substrate 4-propargyloxy-2-hydroxy acetophenone using a set of different reactions has been developed. The chalcones and flavanones were screened against mycobacterial FAS-II pathway using a recombinant mycobacterial strain, against which the most potent compound showed ¡«88 % inhibition in bacterial growth and substantially induction of reporter gene activity at 100 ¦ÌM concentration. The triazolylmethoxy aminopyrimdines were screened against PknG of Mycobaceterium tuberculosis displaying moderate to good activity (23-53 % inhibition at 100 ¦ÌM), comparable to the action of a standard inhibitor.