Structure-Based Design of Benzimidazole Sugar Conjugates: Synthesis, SAR and In Vivo Anti-inflammatory and Analgesic Activities
摘要：
A series of 2-methyl-N-substituted-benzimidazoles, bearing hydroxypyrrolidinon-5-yl or hydroxypyrrolidin-2- yl, 2,3:5,6-di-O-isopropylidene-±-D-mannofuranoside, 2,3,5,6-tetrahydroxy-±-D-mannofuranoside, 1:2,5:6-di-O-isopropylidene- ±-D-gluco-furanose,3-O-benzyl-6,7-dideoxy-1:2-O-isopropylidene-±-D-xylo-heptofuranos-5-ulose, 3-O-benzyl- 6,7-dideoxy-1,2-dihydroxy-±-D-xylo-heptofuranos-5-ulose, 1,2,5,6-tetrahydroxy-±-D-glucofuranose sugar moieties, were obtained in good yields from 2-methyl N-(trichloroacetamidomethyl)benzimidazole as a donor and carbohydrate residues as acceptor precursors in the presence of catalytic amount of trimethylsilyl trifluoromethanesulfonate (TMSOTf) as Lewis acid. Compounds 6, 7, 10, 13, 15, and 16 showed significant anti-inflammatory and analgesic activities.
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DOI：
10.2174/157340609790170461
被引量：
年份：
2009
国家科技图书文献中心
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掌桥科研
Ingenta
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NCBI
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