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Bioorg Med Chem Lett. 2013 Jan 1;23(1):291-6. doi: 10.1016/j.bmcl.2012.10.101. Epub 2012 Nov 1.

A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents.

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1
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226001, India.

Abstract

A natural product inspired molecular hybridization approach led us to a series of novel pentamidine based pyrimidine and chalcone scaffolds. All the hybrids were evaluated for their anti-leishmanial potential. Most of the screened compounds have showed significant in vitro anti-leishmanial activity with less cytotoxicity in comparison to the standard drugs (pentamidine, sodium stibogluconate, and miltefosine). Additionally, anti-malarial screening of these compounds was also done and four compounds have shown superior activity against chloroquine resistance strain (K1) of Plasmodium falciparum.

PMID:
23182089
DOI:
10.1016/j.bmcl.2012.10.101
[Indexed for MEDLINE]
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