New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents
نویسندگان
چکیده
منابع مشابه
InhA Inhibitors as Potential Antitubercular Agents (A Review)
Infectious diseases pose a potential threat and are responsible for killing more people globally than any other single cause. For six decades, antibiotics have been a bulwark against bacterial infectious diseases. This bulwark is failing due to the appearance of resistant bacterial strains. The biosynthesis pathway of fatty acids in bacteria represents a validated target for antibacterial drug ...
متن کاملNew Insight into the SAR of Pyrimido [4,5-b][1,4] Benzothiazines as 15-lipoxygenase Inhibitors
Objective(s): Recently we reported that the soybean 15-lipoxygenase (SLO) inhibitory activity of pyrimido[4,5-b][l,4]benzothiazines largely depends on the orientation of sulfur atom of thiazine core towards FeIII-OH in the active site pocket of the enzyme with subsequent oxidation of sulfur to sulfoxide. In this paper the results of a comparative study on the SLO inhibitory activities of the ...
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Novel drugs to treat tuberculosis are required and the identification of potential targets is important. Piperidinols have been identified as potential antimycobacterial agents (MIC < 5 μg/mL), which also inhibit mycobacterial arylamine N-acetyltransferase (NAT), an enzyme essential for mycobacterial survival inside macrophages. The NAT inhibition involves a prodrug-like mechanism in which acti...
متن کاملnew insight into the sar of pyrimido [4,5-b][1,4] benzothiazines as 15-lipoxygenase inhibitors
objective(s): recently we reported that the soybean 15-lipoxygenase (slo) inhibitory activity of pyrimido[4,5-b][l,4]benzothiazines largely depends on the orientation of sulfur atom of thiazine core towards feiii-oh in the active site pocket of the enzyme with subsequent oxidation of sulfur to sulfoxide. in this paper the results of a comparative study on the slo inhibitory activities of the me...
متن کاملSynthesis of Isoxazoles and Cyanopyridines Bearing Benzo(b)thiophene Nucleus as Potential Antitubercular and Antimicrobial Agents
Isoxazole (2a-l) and cyanopyridine (3a-l) derivatives have been prepared by condensing chalcones (1a-l) with hydroxylamine hydrochloride and malononitrile respectively. While compounds 1a-l have been synthesized by the reaction of p-(3’-chloro-2’-benzo(b)thiophenoylamino)-acetophenone with different aldehydes. All the compounds were screened for their antitubercular and antimicrobial activities...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2019
ISSN: 1475-6366,1475-6374
DOI: 10.1080/14756366.2019.1589462