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J Enzyme Inhib Med Chem. 2016 Dec;31(6):1146-55. doi: 10.3109/14756366.2015.1101094. Epub 2015 Nov 2.

Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads.

Author information

1
a Institutes of Chemistry and Translational Biomedicine, Saint Petersburg State University , Saint Petersburg , Russian Federation .
2
b Eskitis Institute for Drug Discovery, Griffith University , Brisbane , Queensland , Australia .
3
c Chemical Diversity Research Institute , Khimki, Moscow Region , Russian Federation , and.
4
d Saint Petersburg Research Institute of Phthisiopulmonology , Saint Petersburg , Russian Federation.

Abstract

A novel library based on quinolin-4-ylimidazoline core was designed to incorporate a general quinoline antimicrobial pharmacophore. A synthesis of the well-characterized library of 36 compounds was achieved using the Pd-catalyzed Buchwald-Hartwig-type imidazoline arylation chemistry developed earlier. Compounds were tested for biological activity and were found to possess no antimalarial activity. However, the library delivered two promising antitubercular leads, which are non-cytotoxic and can be further optimized with respect to antimycobacterial potency.

KEYWORDS:

2-imidazoline; Antimalarial; Buchwald–Hartwig; antitubercular; microwave chemistry; non-cytotoxic; quinoline

PMID:
26526717
DOI:
10.3109/14756366.2015.1101094
[Indexed for MEDLINE]

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