Design, synthesis and biological evaluation of piperazinyl-β-carbolinederivatives as anti-leishmanial agents
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Molecular hybridization is a ligand based drug design approach is well known recent medicinal chemistry to design anti-parasitic agents. In the present study, we have designed a series of (1-phenyl-9H-pyrido [3,4-b]indol-3-yl) (4-phenylpiperazin-1-yl)methanone derivatives using molecular hybridization approach. Designed analogues were evaluated for cytotoxicity and inhibition activity against Leishmania infantum and Leishmania donovani. Among these reported analogues 7b , 7d , 7e , 7f and 7m displayed potent inhibition of both L. infantum and L. donovani. Compounds 7i and 7k exhibited selective potent inhibition of L. donovani. Especially, compounds 7e and 7k showed most potent anti-leishmanial activity against L. infantum and L. donovani respectively. Anti-leishmanial activity of these compounds is comparable with standard drugs miltefosine and pentamidine. SAR studies revealed that, electron donating group substitution on phenyl ring recommended for potent anti-leishmanial activity.
Ashok , P , Chander , S , Smith , T K & Sankaranarayanan , M 2018 , ' Design, synthesis and biological evaluation of piperazinyl-β-carbolinederivatives as anti-leishmanial agents ' , European Journal Of Medicinal Chemistry , vol. 150 , pp. 559-566 . https://doi.org/10.1016/j.ejmech.2018.03.022
European Journal Of Medicinal Chemistry
© 2018 Elsevier Masson SAS. This work has been made available online in accordance with the publisher’s policies. This is the author created, accepted version manuscript following peer review and may differ slightly from the final published version. The final published version of this work is available at https://doi.org/10.1016/j.ejmech.2018.03.022
DescriptionOne of the authors, Ashok Penta, acknowledges Council of Scientific and Industrial Research, New Delhi, India for financial support in the form of Senior Research Fellowship. Other authors gratefully acknowledge BITS-Pilani for providing the necessary facilities to do this work. This work was carried out under a grant from Science and Engineering Research Board of Department of Science and Technology, New Delhi. (Ref. No: SR/FT/LS-58/2011). This work was also partially supported by TKS's Welcome Trust project grant 093228 and the European Community's Seventh Framework Program under grant agreement No.602773 (Project KINDRED).
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