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Literature DB >> 20932608

Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives.

Raoni S B Gonçalves¹, Carlos R Kaiser, Maria C S Lourenço, Marcus V N de Souza, James L Wardell, Solange M S V Wardell, Adilson D da Silva.

Abstract

In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory concentration (MIC) in μM. The compounds were non-cytotoxic and exhibited an important activity (12.6 μM). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds.

Entities: Chemical Gene

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Year: 2010 PMID： 20932608 DOI： 10.1016/j.ejmech.2010.09.024

Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514

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Cited

6 in total

1. Second generation of primaquine ureas and bis-ureas as potential antimycobacterial agents.

Authors: Kristina Pavić; Zrinka Rajić; Hana Michnová; Josef Jampílek; Ivana Perković; Branka Zorc
Journal: Mol Divers Date: 2018-12-06 Impact factor: 2.943

2. One-Pot Synthesis, Spectroscopic and Physicochemical Studies of Quinoline Based Blue Emitting Donor-Acceptor Chromophores with Their Biological Application.

Authors: Abdullah M Asiri; Salman A Khan; Saad H Al-Thaqafya
Journal: J Fluoresc Date: 2015-08-25 Impact factor: 2.217

Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives.

1. Second generation of primaquine ureas and bis-ureas as potential antimycobacterial agents.

2. One-Pot Synthesis, Spectroscopic and Physicochemical Studies of Quinoline Based Blue Emitting Donor-Acceptor Chromophores with Their Biological Application.

3. 2-{1-[2,8-Bis(trifluoro-meth-yl)quinolin-4-yl]-3,5,6,7,8,8a-hexa-hydro-1H-1,3-oxazolo[3,4-a]pyridin-3-yl}phenol.

4. Benzyl 2-{[2,8-bis-(trifluoro-meth-yl)quinolin-4-yl](hy-droxy)meth-yl}piperidine-1-carboxyl-ate.

5. tert-Butyl 2-{[2,8-bis-(trifluoro-meth-yl)quinolin-4-yl](hy-droxy)meth-yl}piperidine-1-carboxyl-ate.

Review 6. A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine.