期刊
ADVANCED SYNTHESIS & CATALYSIS
卷 353, 期 10, 页码 1787-1796出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201100288
关键词
antipyretic agents; asymmetric synthesis; methylthioimidazolines; tertiary amine-thiourea catalysts
资金
- National Natural Science Foundation of China [20932003, 90813012]
- Ministry of Science and Technology of China [2009ZX09503-017]
- Fundamental Research Funds for the Central Universities of China [860618]
Drug lead synthesis by the rapid construction of chiral molecular complexity around the biologically relevant framework using a highly efficient strategy is a key goal of organic synthesis. Herein, a highly efficient and convenient strategy that allows the rapid synthesis of highly optically active methylthioimidazolines through the novel rosin-derived thiourea-catalyzed asymmetric synthesis of cyclic thioureas with high levels of enantio- and diastereoselectivity (up to 99% ee, and 20:1 dr) via Mannich reaction is described fior the first time. Several of the new methylthioimidazolines showed extremely promising antipyretic activity in the development of neuroinflammation through preliminary biological studies. Additionally, to gain a better understanding of the structural stability-activity relationships, explicit molecular dynamics (MD) simulations in water at room temperature and at body temperature were investigated.
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