Synthesis, spectral characterization, and antituberculosis activity of thiazino[3,2-<i>A</i>]benzimidazole derivatives

Abstract

ABSTRACTA series of novel thiazino[3,2-a]benzimidazole derivatives synthesized by cyclization of (R)-2-(chloromethyl)oxirane with benzimidazole-2-thiol followed by reacted with benzyl bromides in high yield under milder conditions. The molecular structures of all compounds were confirmed by 1H and 13C NMR spectroscopy and Mass spectrometry. The absolute configuration of the compounds was confirmed by X-ray diffraction analysis. All the synthesized compounds were evaluated in vitro for their antituberculosis activity. KEYWORDS: Thiazino-benzimidazole derivativessynthesiscrystal structureanti-TB activity FundingThis research work was financially supported by the Natural Science Foundation of China (Nos. 81520108028, 81273430, 41306130, 41506187, 81302692, 41476063), NSFC-Shandong Joint Fund for Marine Science Research Centers (Grant No. U1406402), SCTSM Project (Nos. 14431901100, 15431901000), and the SKLDR/SIMM Projects (CASIMM0120152039, SIMM1501ZZ-03).