Published on September 2012 | Anti mycobacterial, Synthetic chemistry, Drug screening, tuberculosis, Lipid metabolism, FAS-II, PknG

Synthesis and evaluation of small libraries of triazolylmethoxy chalcones, flavanones and 2-aminopyrimidines as inhibitors of mycobacterial FAS-II and PknG
Authors: Namrata Anand, Priyanka Singh, Anindra Sharma, Sameer Tiwari, Vandana Singh, Diwakar K Singh, Kishore K Srivastava, B N Singh, Rama Pati Tripathi
View Author: Dr. VANDANA SINGH
Journal Name: Bioorganic & medicinal chemistry
Volume: 20 Issue: 17 Page No: 5150-5163
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Abstract:

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 μM concentration. The triazolylmethoxy aminopyrimdines were screened against PknG of Mycobaceterium tuberculosis displaying moderate to good activity (23-53% inhibition at 100 μM), comparable to the action of a standard inhibitor.

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