Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives

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

doi:10.1016/j.ejmech.2010.09.024

Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives

Eur J Med Chem. 2010 Dec;45(12):6095-100. doi: 10.1016/j.ejmech.2010.09.024. Epub 2010 Sep 17.

Authors

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

Affiliation

¹ FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.

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

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.

MeSH terms

Antitubercular Agents / chemical synthesis
Antitubercular Agents / chemistry
Antitubercular Agents / pharmacology*
Crystallography, X-Ray
Drug Design
Mefloquine / chemical synthesis
Mefloquine / chemistry
Mefloquine / pharmacology*
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Mycobacterium tuberculosis / drug effects*
Oxazoles / chemical synthesis
Oxazoles / chemistry
Oxazoles / pharmacology*
Structure-Activity Relationship

Substances

Antitubercular Agents
Oxazoles
oxazolidine
Mefloquine