2. Academic Validation
  3. Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors

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

  • Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7. doi: 10.1016/j.bmcl.2003.08.056.
Scott D Edmondson 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. scott_edmondson@merck.com
PMID: 14592490 DOI: 10.1016/j.bmcl.2003.08.056
Abstract

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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