从 D-葡萄糖合成多种糖基化脲类并进行抗结核评价

IF 2.8 4区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Neetu Tripathi, Vinod K. Tiwari
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引用次数: 0

摘要

通过将胺与糖基化烯烃酯进行 1,4 共轭加成,然后将生成的糖基化 β-氨基酯与二异氰酸酯反应,合成了 N,N-二取代的糖基化脲。通过广泛的标准光谱分析,包括核磁共振(1H、13C 和 DEPT)、红外光谱、质谱和元素分析,对所开发的糖基分子进行了充分的表征,并对其抗结核分枝杆菌(M. Tb.)的生物活性进行了筛选,其中一些分子显示出了强大的抗结核活性。这些分子的设计考虑到了参与分枝杆菌细胞壁聚合物生物合成的众所周知的酶抑制剂,可进一步作为先导分子进行探索,以成功开发潜在的抗结核候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and Antitubercular Evaluation of Diverse Glycosylated Ureas from D-Glucose
N, N-disubstituted glycosylated ureas have been synthesized in good-to-excellent yields by 1,4-conjugate addition of amines to glycosylated olefinic esters followed by reaction of resulting glycosyl β-amino esters with diisocyanates. The developed sugar-based molecules were well characterized by extensive standard spectroscopic analysis including NMR (1H, 13C, and DEPT), IR, MS, and elemental analysis and were screened for their biological activity against Mycobacterium tuberculosis (M. Tb.), where some of them displayed potent antitubercular activity. The molecules have been designed keeping in view the well-known inhibitors of the enzymes involved in the biosynthesis of mycobacterial cell wall polymers and may be further explored as lead molecules for the successful development of a potential antitubercular drug candidate.
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来源期刊
Journal of Chemistry
Journal of Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
5.90
自引率
3.30%
发文量
345
审稿时长
16 weeks
期刊介绍: Journal of Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry.
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