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Haonan Li,Baojia Sun,Mingying Wang,Xu Hu,Xiang Gao,Sheng-tao Xu,Yongnan Xu,Jin-yi Xu,Hui-Ming Hua,Da-Hong Li 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.11
Diterpenoids are important and widely distributed natural compounds with various biological effects, including antitumor, anti-inflammatory and so on. Great efforts have been put in phytochemistry research on diterpenoids. A number of structural modified derivatives and pharmacophore incorporated hybrids were also designed and synthesized with promising therapeutic effects. Among the hopefuls, enmein-type 6,7-seco-ent-kaurane diterpenoids with unique ring system and stereogenic centers exhibit attractive activities. Based on their lead-like properties, enmein-type diterpenoids are suitable for further medicinal study. The derivatives were biologically evaluated and showed promising activities, which warranted in-depth research for further understanding. In this review, the natural bioactive enmein-type diterpenoids and the synthetic derivatives were comprehensively summarized.
A New Triterpenoid Saponin from Pulsatilla cernua
Wenhao Fan,Yongnan Xu,Jianyu Liu,Yixia Gong,Jing Ma,Nan Zhou 한국생약학회 2013 Natural Product Sciences Vol.19 No.2
A new oleanane-type triterpenoid saponin together with six known saponins were isolated from the roots of Pulsatilla cernua. Their structures were elucidated on the basis of spectroscopic data, including 2D NMR spectra and chemical evidence. Compounds 1 and 6 are reported from this genus for the first time.
Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
Yu-Juan Zhang,Liu-Lan Shen,천혜경,Yongnan Xu,정진현 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.5
In this study, a series of fused-heterocyclicderivatives were systematically designed and synthesizedusing an efficient route, and evaluated in terms of GLP-1Ragonist activity. We employed short synthetic steps andreactions that are tolerant of the presence of variousfunctional groups and suitable for parallel operations toenable the rapid generation of libraries of diverse andstructurally complex small molecules. Of the compoundssynthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)phenyl methanesulfonate (8e) was the mostpotent agonist with an EC50 of 7.89 lM, and thus is thecompound with the greatest potential for application. Thesefindings represent a valuable starting point for the designand discovery of small-molecule GLP-1R agonists that canbe administered orally.