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Molecules 2012, 17(12), 14522-14530; doi:10.3390/molecules171214522

Synthesis and Antiviral Activity of Conformational Analogues of Leucamide A

1,*  and 2,*
1 School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China 2 Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences, Graduate School of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, China
* Authors to whom correspondence should be addressed.
Received: 1 November 2012 / Revised: 28 November 2012 / Accepted: 30 November 2012 / Published: 7 December 2012
(This article belongs to the Section Medicinal Chemistry)
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In order to study the effect of heterocyclic core conformational state of leucamide A on its anti-influenza virus A activity, five conformational analogues were prepared by replacing the Pro-Leu dipeptide in the molecule with various amino acids. The amino acids used were of 2 to 6 carbons. The results showed that these replacements not only changed the conformational relationship between the 4,2-bisheterocycle tandem pair and the third heterocycle, but also had dramatic effect on its activity against influenza virus A.
Keywords:  leucamide A; conformational analogues; synthesis; anti-influenza virus A  ; leucamide A; conformational analogues; synthesis; anti-influenza virus A
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Wang, W.-L.; Chen, H.-J.; Ma, W.-P.; Gu, M.; Fan, M.-Z.; Li, J.-Y.; Feng, B.; Nan, F.-J. Synthesis and Antiviral Activity of Conformational Analogues of Leucamide A. Molecules 2012, 17, 14522-14530.

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