Abstract
The condensation of chlorides of substituted pyrazinecarboxylic acids with ring-substituted anilines yielded twelve substituted pyrazinecarboxylic acid amides. The synthetic approach, analytical, and lipophilicity data of the newly synthesized compounds are presented. Two antituberculosis assays were used. Firstly, the antimycobacterial activity against four different Mycobacterium strains in a series of pyrazine derivatives was investigated. Secondly, the antimycobacterial evaluation was performed at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) program. Interesting in vitro antimycobacterial activity was found, N-(3-iodo-4-methyl-phenyl)pyrazine-2-carboxamide (9) was most active derivative compound against M. tuberculosis (MIC < 2.0 μmol/L), while another iodo derivative 5-tert-butyl-6-chloro-N-(3-iodo-4-methyl-phenyl)pyrazine-2-carboxamide (12) was the most active compound in the TAACF antituberculosis screening program (IC90 = 0.819 µg/mL).
Highlights
Every year, tuberculosis (TB) kills some 3.1 million people, more deaths than those caused by any other single bacterial disease
Drug Resistance, XDR-TB) is MDR-TB that is resistant to three or more of the six classes of second-line drugs. This follows research showing the extent of XDR-TB, a newly identified TB threat which leaves patients virtually untreatable using currently available anti-TB drugs
This paper deals with structure-activity relationship (SAR) of some PZA analogues derived from binuclear compounds with the -CONH- linker
Summary
Tuberculosis (TB) kills some 3.1 million people, more deaths than those caused by any other single bacterial disease. The World Health Organization has expressed concern over the emergence of virulent drug-resistant strains of TB and is calling for measures to be strengthened and implemented to prevent the global spread of these deadly TB strains. Multidrug Resistant TB (MDRTB) describes strains of tuberculosis that are resistant to at least the two main first-line TB drugs—isoniazid (INH) and rifampicin. Drug Resistance, XDR-TB) is MDR-TB that is resistant to three or more of the six classes of second-line drugs. This follows research showing the extent of XDR-TB, a newly identified TB threat which leaves patients (including many people living with HIV) virtually untreatable using currently available anti-TB drugs. An urgent need is to develop new agents active against resistant bacteria, and having different mechanism of action [1,2]
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