Synthesis of N-heterocyclic carbene boranes via silver N-heterocyclic carbene complexes
The reaction of N-heterocyclic carbene (NHC) complexes of silver with BH3 or BEt3 was investigated. On treatment of IiPr·AgCl (1-AgCl) (IiPr = 1,3-diisopropylimidazol-2-ylidene) with two equivalents of NaBH
An efficient and environmental benign synthesis of 2-benzimidazoles and 2-benzothiazoles using CeCl3-NaI as catalyst
A one-pot condensation of an aldehyde with 1,2-phenylenediamine or 2-aminothiophenol in dimethyl carbonate at 100°C under O2 in the presence of catalytic amounts of CeCl3-NaI gave an imine intermediate, which cyclised and dehydrogenated to give 2-arylbenzimidazoles or 2-arylbenzothiazoles in good yields.
Zhu, Xun,Wei, Yunyang
p. 119 - 121
(2013/04/23)
Inhibitors of the salicylate synthase (Mbti) from Mycobacterium tuberculosis discovered by high-throughput screening
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.
Vasan, Mahalakshmi,Neres, Joao,Williams, Jessica,Wilson, Daniel J.,Teitelbaum, Aaron M.,Remmel, Rory P.,Aldrich, Courtney C.
experimental part
p. 2079 - 2087
(2011/11/29)
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