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Synthesis and evaluation of novel chromanone and quinolinone analogues of uniflorol as anti-leishmanial agents.
Castro, Helena Cruz, Tânia de Aguiar Amaral, Patrícia da Silva Cardoso, Paula Alsaffar, Ahmed Farrell, Patrick Tomás, Ana M Barlow, James W
Castro, Helena
Cruz, Tânia
de Aguiar Amaral, Patrícia
da Silva Cardoso, Paula
Alsaffar, Ahmed
Farrell, Patrick
Tomás, Ana M
Barlow, James W
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Date
2020-03-20
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Keywords
Chromanone
Leishmania
Natural product chemistry
Organic chemistry
Pharmaceutical chemistry
Quinolinone
Leishmania
Natural product chemistry
Organic chemistry
Pharmaceutical chemistry
Quinolinone
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Abstract
Within this work, we describe the design and synthesis of a range of novel chromanones and quinolinones, based on natural products reported to possess anti-leishmanial action. The core heterocycles were obtained either via classical or ionic liquid mediated Kabbe condensation in the case of chromanones, or aqueous Sonogashira based alkynylation followed by acid-catalysed cyclisation in the case of quinolinones. Upon testing in promastigotes, axenic amastigotes and Leishmania-infected macrophages, compound 13c was identified as displaying interesting activity, inhibiting axenic amastigotes and intracellular amastigotes with IC50s of 25.3 and 24.6μM respectively.
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en
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ISSN
2405-8440
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DOI
10.1016/j.heliyon.2020.e03614
PMID
32258470