A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents |
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| Authors: | Vikas Tyagi Shahnawaz Khan Rahul Shivahare Khushboo Srivastava Suman Gupta Saqib Kidwai Kumkum Srivastava S.K. Puri Prem M.S. Chauhan |
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| Affiliation: | 1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226001, India;2. Parasitology Division, CSIR-Central Drug Research Institute, Lucknow 226001, India |
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| 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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