title: Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads.
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.
authors.affiliation: a Institutes of Chemistry and Translational Biomedicine, Saint Petersburg State University , Saint Petersburg , Russian Federation .
authors.forename: Mikhail
authors.initials: M
authors.lastname: Krasavin
authors.affiliation: b Eskitis Institute for Drug Discovery, Griffith University , Brisbane , Queensland , Australia .
authors.forename: Prashant
authors.initials: P
authors.lastname: Mujumdar
authors.affiliation: c Chemical Diversity Research Institute , Khimki, Moscow Region , Russian Federation , and.
authors.forename: Vladislav
authors.initials: V
authors.lastname: Parchinsky
authors.affiliation: d Saint Petersburg Research Institute of Phthisiopulmonology , Saint Petersburg , Russian Federation.
authors.forename: Tatiana
authors.initials: T
authors.lastname: Vinogradova
authors.affiliation: d Saint Petersburg Research Institute of Phthisiopulmonology , Saint Petersburg , Russian Federation.
authors.forename: Olga
authors.initials: O
authors.lastname: Manicheva
authors.affiliation: d Saint Petersburg Research Institute of Phthisiopulmonology , Saint Petersburg , Russian Federation.
authors.forename: Marine
authors.initials: M
authors.lastname: Dogonadze
mesh_terms: D000995:Antitubercular Agents / Q000008:administration & dosage*; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D002384:Catalysis; D048288:Imidazolines / Q000008:administration & dosage*; D010165:Palladium / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000995:Antitubercular Agents; D048288:Imidazolines; D010165:Palladium
keywords: 2-imidazoline; Antimalarial; Buchwald–Hartwig; antitubercular; microwave chemistry; non-cytotoxic; quinoline