Synthesis,spectral characterization,and antituberculosis activity of thiazino[3,2-A]benzimidazole derivatives |
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Authors: | Jing-Xu Gong Zhen-Lin Cui |
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Institution: | 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China;2. Clinic and Research Center of Tuberculosis, Shanghai Key Lab of Tuberculosis, Shanghai Pulmonary Hospital, School of Medicine, Tongji University, Shanghai, China |
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Abstract: | A series of novel thiazino3,2-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. |
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Keywords: | Thiazino-benzimidazole derivatives synthesis crystal structure anti-TB activity |
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