2-substituted 4-, 5-, and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as potent platelet aggregation inhibitors:: Design, synthesis, and SAR studies

被引：13

作者：

Meyers, Caroline ^{[1
]}

Yanez, Matilde ^{[2
]}

Elmaatougi, Abdelazlz ^{[3
]}

Verhelst, Tom ^{[1
]}

Coelho, Alberto ^{[4
]}

Fraiz, Nuria ^{[2
]}

Lemiere, Guy L. F. ^{[1
]}

Garcia-Mera, Xerardo ^{[3
]}

Laguna, Reyes ^{[2
]}

Cano, Ernesto ^{[2
]}

Maes, Bert U. W. ^{[1
]}

Sotelo, Eddy ^{[3
,4
]}

机构：

[1] Univ Antwerp, Dept Chem, B-2020 Antwerp, Belgium

[2] Univ Santiago Compostela, Fac Pharm, Dept Farmacol, Espana, Spain

[3] Univ Santiago Compostela, Fac Pharm, Dept Quim Organ, Espana, Spain

[4] Univ Santiago Compostela, IFI, Unidad Quim Combinatoria, Espana, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 02期

关键词：

platelets; pyridazinones; chalcones; antiplatelet agents;

D O I：

10.1016/j.bmcl.2007.11.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A set of regioisomeric 2-substituted pyridazin-3(2H)-ones containing a 3-oxo-3-phenylprop-1-en-1-yl fragment at either position 4, 5 or 6 and 2-substituted pyridazin-3(2H)-ones containing the same fragment both at positions 4 and 5 have been synthesized and evaluated as antiplatelet agents. The study allows the identification of a new highly potent platelet aggregation inhibitor (4c). (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：793 / 797

页数：5

共 44 条

[1] INOTROPIC, VASODILATOR AND LOW KM, CAMP-SELECTIVE, CGMP-INHIBITED PHOSPHODIESTERASE (PDE III) INHIBITORY ACTIVITIES OF 4-ALPHA-METHYL-4,4-ALPHA-DIHYDRO-5H-INDENO[1,2-C]PYRIDAZIN-3(2H)-ONES AND 4-ALPHA-METHYL-4,4-ALPHA,5,6-TETRAHYDROBENZO[H]CINNOLIN-3(2H)-ONES [J].