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Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.

ABSTRACT: The influence of various structural patterns in a series of novel bi- and tricyclic N-heterocycles on the activity against Leishmania major and Leishmania panamensis has been studied and compounds that are active in the low micromolar region have been identified. Both quinolines and tetrahydrooxazinoindoles (TOI) proved to have significant antileishmanial activities, while substituted indoles were inactive. We have also showed that a chloroquine analogue induces Leishmania killing by modulating macrophage activation.

SUBMITTER: Herrera L

PROVIDER: S-EPMC4958403 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature

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Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.

Herrera Lizzi L Stephens David E DE D'Avila Abigail A George Kathryn G KG Arman Hadi H Zhang Yu Y Perry George G Lleonart Ricardo R Larionov Oleg V OV Fernández Patricia L PL

Organic & biomolecular chemistry 20160704 29

The influence of various structural patterns in a series of novel bi- and tricyclic N-heterocycles on the activity against Leishmania major and Leishmania panamensis has been studied and compounds that are active in the low micromolar region have been identified. Both quinolines and tetrahydrooxazinoindoles (TOI) proved to have significant antileishmanial activities, while substituted indoles were inactive. We have also showed that a chloroquine analogue induces Leishmania killing by modulating ...[more]

PMID: 27376396

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