alexa 3,5-Dibromo-2,4-dihydroxy Substituted Chalcones: Synthesis and in vitro Trypanocidal Evaluation | OMICS International
ISSN: 2161-0401

Organic Chemistry: Current Research
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Research Article

3,5-Dibromo-2,4-dihydroxy Substituted Chalcones: Synthesis and in vitro Trypanocidal Evaluation

K. L. Ameta1*, Nitu S. Rathore1, Biresh Kumar1, Edith S. Maalaga M2, Manuela Veraastegui2 and Robert H. Gilman3
1Department of Chemistry, FASC, Mody Institute of Technology & Science, Lakshmangarh-332311, Rajasthan, India
2Department of Microbiology, Faculty of Science and Philosophy, Universidad Peruana Cayetano Heredia, Lima, Peru
3Department of International Health, Bloomberg School of Public Health, Johns Hopkins University, Baltimore, Maryland-21205, USA
Corresponding Author : K. L. Ameta
Department of Chemistry
Faculty of Arts Science and Commerce (FASC)
MITS University, Lakshmangarh
Sikar, Rajasthan-332311 India
Tel: +91-9414682501
Fax: +91-1573225044
E-mail: [email protected], [email protected]
Received July 11, 2012; Accepted August 16, 2012; Published August 20, 2012
Citation: Ameta KL, Rathore NS, Kumar B, Maalaga MES, Veraastegui M, et al. (2012) 3′,5′-Dibromo-2′,4′-dihydroxy Substituted Chalcones: Synthesis and in vitro Trypanocidal Evaluation. Organic Chem Curr Res 1:107. doi:10.4172/2161-0401.1000107
Copyright: © 2012 Ameta KL, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

A new series of 3′, 5′-dibromo-2′, 4′-dihydroxy substituted chalcones was synthesized by the classical Claisen- Schmidt condensation of 3, 5-dibromo-2, 4-dihydroxyacetophenone and variously substituted aromatic aldehydes via conventional as well as non-conventional inorganic solid supported microwave irradiation methods. The non- conventional methodology, has the advantages of being rapid, eco-friendly, easy to handle, requiring shorter reaction time, and quite general. All newly synthesized compounds were evaluated for their inhibitory effect against Trypanosoma cruzi (Chagas disease). Compounds 3c, 3g and 3m showed 85.53, 85.03 and 83.34 in-vitro percentage growth of inhibition respectively; while compounds 3b, 3e, 3i and 3l showed 71.23, 71.95, 67.53 and 68.88 percentage growth of inhibition respectively with nifurtimox and benznidazole as reference drugs. 3l was the compound with a good anti- trypanocidal activity, the lower cytotoxicity, higher therapeutic index 14.5, and was the best candidate in comparison with the others. The structures of the newly synthesized compounds (3a-t) were determined by elemental analysis, FTIR, 1H-NMR, 13C-NMR and mass spectroscopic studies.

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