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Molecules 2008, 13(2), 432-443; doi:10.3390/molecules13020432
Article

Synthesis and Antimalarial Evaluation of Cyclic β-Amino Acid-Containing Dipeptides

1, 2, 1 and 1,*
1 Discovery Center, Defence R & D Establishment, Jhansi Road, Gwalior 474002, India. 2 Microbiology Division, Defence Research and Development Establishment, Gwalior-474002, India
* Author to whom correspondence should be addressed.
Received: 31 January 2008 / Revised: 11 February 2008 / Accepted: 15 February 2008 / Published: 18 February 2008
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Abstract

This paper describes an efficient synthesis and the antiparasitic evaluation ofcyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial propertiesof all these dipeptides have been evaluated in vitro against Plasmodium falciparum and invivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be veryeffective in this respect, with IC50 values of 3.87 and 3.64 μg/mL in the in vitro test, while4.5 has also been found to be active in the in vivo evaluation.
Keywords: β-Lactam; β-amino acid; antimalarial; Plasmodium falciparum; Plasmodium berghai β-Lactam; β-amino acid; antimalarial; Plasmodium falciparum; Plasmodium berghai
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Sathe, M.; Thavaselvam, D.; Srivastava, A.K.; Kaushik, M.P. Synthesis and Antimalarial Evaluation of Cyclic β-Amino Acid-Containing Dipeptides. Molecules 2008, 13, 432-443.

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