| Literature DB >> 24139881 |
Valnês S Rodrigues-Junior1, André A dos Santos Junior2, Anne D Villela2, Juan M Belardinelli3, Héctor R Morbidoni3, Luiz A Basso1, Maria M Campos4, Diógenes S Santos5.
Abstract
In this work, the antitubercular activity of a pentacyano(isoniazid)ferrate(II) compound (IQG-607) was investigated using a macrophage model of Mycobacterium tuberculosis infection. Importantly, treatment of M.-tuberculosis-infected macrophages with IQG-607 significantly diminished the number of CFU compared with the untreated control group. The antitubercular activity of IQG-607 was similar to that observed for the positive control drugs isoniazid and rifampicin. Nevertheless, higher concentrations of IQG-607 produced a significantly greater reduction in bacterial load compared with the same concentrations of isoniazid. Analysis of the mechanism of action of IQG-607 revealed that the biosynthesis of mycolic acids was blocked. The promising activity of IQG-607 in infected macrophages and the experimental determination of its mechanism of action may help in further studies aimed at the development of a new antimycobacterial agent.Entities:
Keywords: Drug development; IQG-607; Mycolic acid biosynthesis inhibitor; Tuberculosis
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Year: 2013 PMID: 24139881 DOI: 10.1016/j.ijantimicag.2013.08.021
Source DB: PubMed Journal: Int J Antimicrob Agents ISSN: 0924-8579 Impact factor: 5.283