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

被引：36

作者：

Edmondson, SD

Mastracchio, A

He, JF

Chung, CC

Forrest, MJ

Hofsess, S

MacIntyre, E

Metzger, J

O'Connor, N

Patel, K

Tong, XC

Tota, MR

Van der Ploeg, LHT

Varnerin, JP

Fisher, MH

Wyvratt, MJ

Weber, AE

Parmee, ER

机构：

[1] Merck & Co Inc, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Metab Disorders, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Pharmacol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 22期

关键词：

D O I：

10.1016/j.bmcl.2003.08.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC50 = 0.19 nM, 3A IC50 = 1.3 nM) was selected for in vivo evaluation of lipolysis induction, metabolic rate increase, and cardiovascular effects. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：3983 / 3987

页数：5

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