200059-78-5Relevant articles and documents
Peramivir conjugates as orally available agents against influenza H275Y mutant
Wang, Peng-Cheng,Chiu, Din-Chi,Jan, Jia-Tsrong,Huang, Wen-I,Tseng, Yin-Chen,Li, Ting-Ting,Cheng, Ting-Jen,Tsai, Keng-Chang,Fang, Jim-Min
, p. 224 - 234 (2018)
Peramivir is an efficacious neuraminidase (NA) inhibitor for treatment of influenza by intravenous administration. However, the efficacy of peramivir toward the H275Y mutant is appreciably reduced. To address this drawback, conjugation of peramivir with c
TRPV4 activity inhibitor
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, (2020/05/16)
PROBLEM TO BE SOLVED: To provide a compound that inhibits TRPV4 activity and is useful for prevention or improvement of overactive bladder and irritable bowel syndrome or the like. SOLUTION: A TRPV4 activity inhibitor has a rosmarinic acid derivative selected from the formulae (Ia)-(Id) or a salt thereof as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
Synthetic phenylethanoid glycoside derivatives as potent neuroprotective agents
Liu, Ying-Guo,Li, Xiaxi,Xiong, De-Cai,Yu, Binhan,Pu, Xiaoping,Ye, Xin-Shan
, p. 313 - 323 (2015/03/31)
Several phenylethanoid glycoside derivatives were designed and synthesized. Most of the synthetic compounds showed significant neuroprotective effects, including antioxidative and anti-apoptotic properties. Specifically, target compounds displayed potent effects against various toxicities such as H2O2 and 6-hydroxydopamine (6-OHDA) in PC12 cells. Among the synthetic derivatives, three compounds (5, 6, 8) exhibited much superior activities to the marketed drug Edaravone. The compounds were able to prevent the 6-OHDA-induced damage in PC12 cells in a dose-dependent manner. The anti-apoptotic effects could be observed via cell morphological changes. Moreover, the compounds significantly reduced the intracellular ROS increase resulting from 6-OHDA treatment. The preliminary structure-activity relationships were also explored. Compounds 5, 6, 8 may hold the potential as promising neuroprotective agents and new lead compounds for the treatment of neurodegenerative diseases or cerebral ischemia.