학술논문

Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads.
Document Type
Article
Source
Journal of Enzyme Inhibition & Medicinal Chemistry. Dec2016, Vol. 31 Issue 6, p1146-1155. 10p.
Subject
*DRUG design
*DRUG synthesis
*ANTITUBERCULAR agents
*ANTINEOPLASTIC agents
*QUINOLINE
*IMIDAZOLINES
*ANTI-infective agents
*DRUG delivery systems
*THERAPEUTICS
Language
ISSN
1475-6366
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. [ABSTRACT FROM PUBLISHER]