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Anti-Leishmanial Activity of Flavanone Analogues Targeting Pteridine Reductase

By: Afroze Alam.
Contributor(s): Pandit, Vinay | Shailendra Kumar.
Publisher: Bengaluru Association of Pharmaceutical Teachers of India (APTI) 2018Edition: Vol. 52(3), July-September.Description: 480-491.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical education and researchSummary: Objectives: The aim of the study is to develop new synthetic anti-leishmanial agents as flavanone analogues, which should have low toxicity with noticeable yield. Methodology: The starting materials for the synthesis of test compounds were 2’-hydroxypropiohenones, 2’-hydroxyacetophenone and substituted benzaldehyde. Test compounds were synthesized by three steps reaction starting from condensation, cyclization and reduction to yield 3-substituted flananone analogues. The synthesized compounds were screened by in vitro anti-leishmanial assay against promastigotes of L. donovani. Result: A series of flavanone analogues have been synthesized using cobalt (II) phthalocyanine and NaBH4 in the equimolar ratio of the reactant with noticeable yield. The structures of the test compounds were elucidated and established by U.V. IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were screened by in vitro antileishmanial assay against promastigotes of L. donovani. Conclusion: Most of the compounds exhibited moderate leishmanicidal activity, while some compounds such as 4b, 10b, 5b, and 3a have shown promising antileishmanial activity against promastigotes of L. donovani.
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Objectives: The aim of the study is to develop new synthetic anti-leishmanial agents as flavanone analogues, which should have low toxicity with noticeable yield. Methodology: The starting materials for the synthesis of test compounds were 2’-hydroxypropiohenones, 2’-hydroxyacetophenone and substituted benzaldehyde. Test compounds were synthesized by three steps reaction starting from condensation, cyclization and reduction to yield 3-substituted flananone analogues. The synthesized compounds were screened by in vitro anti-leishmanial assay against promastigotes of L. donovani. Result: A series of flavanone analogues have been synthesized using cobalt (II) phthalocyanine and NaBH4 in the equimolar ratio of the reactant with noticeable yield. The structures of the test compounds were elucidated and established by U.V. IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were screened by in vitro antileishmanial assay against promastigotes of L. donovani. Conclusion: Most of the compounds exhibited moderate leishmanicidal activity, while some compounds such as 4b, 10b, 5b, and 3a have shown promising antileishmanial activity against promastigotes of L. donovani.

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