國家衛生研究院 NHRI:Item 3990099045/7706
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    題名: Discovery of 1-(2,4-Dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5 -(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice
    作者: Chang, CP;Wu, CH;Song, JS;Chou, MC;Wong, YC;Lin, Y;Yeh, TK;Sadani, AA;Ou, MH;Chen, KH;Chen, PH;Kuo, PC;Tseng, CT;Chang, KH;Tseng, SL;Chao, YS;Hung, MS;Shia, KS
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: After extensive synthetic efforts, we found that many structurally diverse bioisosteres could be generated via derivatizing the C-4 alkyl chain on the pyrazole ring of compound 3 (B/P = 1/33) with different electronegative groups. Especially when a sulfonamide or sulfamide moiety was added, resulting compounds exhibited not only potent CB1R activity but also a desired tPSA value over 90 A2, a threshold considered to possess a low probability to cross BBB, leading to the identification of compound 4 (B/P = 1/64) as a peripherally restricted CB1R antagonist. Apart from its significant weight-loss efficacy in DIO mice, compound 4 also displays 163 clean off-target profiles and is currently under development for treating obesity and the related metabolic syndrome.
    日期: 2013-11-13
    關聯: Journal of Medicinal Chemistry. 2013 Nov 13;56(24):9920-9933.
    Link to: http://dx.doi.org/10.1021/jm401158e
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000329331600009
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84891281974
    顯示於類別:[夏克山] 期刊論文
    [洪明秀] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [葉燈光] 期刊論文
    [張竣評] 期刊論文

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