2735-73-1Relevant articles and documents
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Cheetham et al.
, p. 729 (1963)
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Inhibitors of the salicylate synthase (Mbti) from Mycobacterium tuberculosis discovered by high-throughput screening
Vasan, Mahalakshmi,Neres, Joao,Williams, Jessica,Wilson, Daniel J.,Teitelbaum, Aaron M.,Remmel, Rory P.,Aldrich, Courtney C.
scheme or table, p. 2079 - 2087 (2011/11/29)
A simple steady-state kinetic high-throughput assay was developed for the salicylate synthase MbtI from Mycobacterium tuberculosis, which catalyzes the first committed step of mycobactin biosynthesis. The mycobactins are small-molecule iron chelators produced by M. tuberculosis, and their biosynthesis has been identified as a promising target for the development of new antitubercular agents. The assay was miniaturized to a 384-well plate format and high-throughput screening was performed at the National Screening Laboratory for the Regional Centers of Excellence in Biodefense and Emerging Infectious Diseases (NSRB). Three classes of compounds were identified comprising the benzisothiazolones (class I), diarylsulfones (class II), and benzimidazole-2-thiones (class III). Each of these compound series was further pursued to investigate their biochemical mechanism and structure-activity relationships. Benzimidazole-2-thione 4 emerged as the most promising inhibitor owing to its potent reversible inhibition.
α-amidoalkylation reactions and oxidation of adducts of benzimidazoles and acyl chlorides
Venkov, Atanas P.,Statkova-Abeghe, Stela
, p. 1857 - 1864 (2007/10/03)
Adducts 4 of benzimidazoles and acyl chlorides were successfully used as electrophilic reagents in an intermolecular α-amidoalkylation reaction toward ketones for synthesis of 2-(2-oxoalkyl)-1,3-diacyl-2,3- dihydrobenzimidazoles 6 and oxidized with KMnO4 to 1,3-diacyl-2,3- dihydrobenzimidazol-2-ones 7.