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

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

  • Bioorg Med Chem Lett. 2013 Jan 1;23(1):291-6. doi: 10.1016/j.bmcl.2012.10.101.
Vikas Tyagi 1 Shahnawaz Khan Rahul Shivahare Khushboo Srivastava Suman Gupta Saqib Kidwai Kumkum Srivastava S K Puri Prem M S Chauhan
Affiliations

Affiliation

  • 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.

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