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

doi:10.3390/molecules13020432

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

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

Manisha Sathe¹, D. Thavaselvam², A. K. Srivastava¹ and M. P. Kaushik^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; in revised form: 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

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MDPI and ACS Style

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.

AMA Style

Sathe M., Thavaselvam D., Srivastava A.K., Kaushik M.P. Synthesis and Antimalarial Evaluation of Cyclic β-Amino Acid-Containing Dipeptides. Molecules. 2008; 13(2):432-443.

Chicago/Turabian Style

Sathe, Manisha; Thavaselvam, D.; Srivastava, A. K.; Kaushik, M. P. 2008. "Synthesis and Antimalarial Evaluation of Cyclic β-Amino Acid-Containing Dipeptides." Molecules 13, no. 2: 432-443.

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