Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.

Scott D Edmondson,Anthony Mastracchio,Jiafang He,Christine C Chung,Michael J Forrest,Scott Hofsess,Euan MacIntyre,Joseph 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

Bioorganic & medicinal chemistry letters（2003）

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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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