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bioRxiv · 10.1101/2020.10.16.342329

A Novel Class of Azoles with potent Anti-Leishmanial activity

Mathur, T.·Kumar, M.·Barman, T. K.·Raj, S. V.·Upadhyay, D. J.·Verma, A. K.
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Abstract

ObjectivesTo investigate the anti-leishmanial activity of novel azole compounds against Leishmania donovani, which causes deadly visceral leishmaniasis disease. MethodsA focused azole-based library was screened both against promastigotes and amastigotes forms of L. donovani strains in flat-bottomed 96-well tissue-culture plates and J774A.1 macrophages infected with L. donovani. The comprehensive screening azole-based library against L. donovani strains provided novel hits, which can serve as a good starting point to initiate hit to lead optimization campaign. ResultsHits identified from azole-based library exhibited potent in vitro activity against promastigotes and amastigotes of L. donovani. ConclusionsThese potent novel azole hits could be a good starting point to carry out for further medicinal chemistry exploration for anti-leishmania program.

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Mathur, T., Kumar, M., Barman, T. K., Raj, S. V., Upadhyay, D. J., Verma, A. K.. 2020-10-16. A Novel Class of Azoles with potent Anti-Leishmanial activity. https://doi.org/10.1101/2020.10.16.342329

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