Synthesis and evaluation of small libraries of triazolylmethoxy chalcones, flavanones and 2-aminopyrimidines as inhibitors of mycobacterial FAS-II and PknG
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Anand, Namrata
Singh, Priyanka Sharma, Anindra Tiwari, Sameer Singh, Vandana Singh, D K Srivastava, K K Singh, B N Tripathi, R P |
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| Date |
2013-03-11T11:02:26Z
2013-03-11T11:02:26Z 2012 |
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| Identifier |
Bioorganic & Medicinal Chemistry 2012, 20 (17), 5150–5163
http://hdl.handle.net/123456789/1033 |
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| Description |
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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1651314 bytes
application/pdf |
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| Language |
en
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| Relation |
CDRI communication no. 8276
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| Subject |
Triazolylmethoxy chalcones
2-Aminopyrimidines Triazolylmethoxy flavanones Mycobacterium tuberculosis FAS-II PknG |
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| Title |
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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| Type |
Article
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