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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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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