化学
酰胺
脂解
体内
立体化学
组合化学
生物化学
生物技术
脂肪组织
生物
作者
Scott D. Edmondson,Anthony Mastracchio,Jiafang He,Caroline Chung,Michael J. Forrest,Scott Hofsess,Euan MacIntyre,Joseph M. Metzger,Naphtali O’Connor,Kajal Patel,Xinchun Tong,Michael R. Tota,Lex H.T. Van der Ploeg,Jeff P. Varnerin,Michael H. Fisher,Matthew J. Wyvratt,Ann E. Weber,Emma R. Parmee
标识
DOI:10.1016/j.bmcl.2003.08.056
摘要
Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC(50)=0.19 nM, 3A IC(50)=1.3 nM) was selected for in vivo evaluation of lipolysis induction, metabolic rate increase, and cardiovascular effects.
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