Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition

被引：10

作者：

Nishida, H ^{[1
]}

Miyazaki, Y ^{[1
]}

Mukaihira, T ^{[1
]}

Shimada, H ^{[1
]}

Suzuki, K ^{[1
]}

Saitoh, F ^{[1
]}

Mizuno, M ^{[1
]}

Matsusue, T ^{[1
]}

Okamoto, A ^{[1
]}

Hosaka, Y ^{[1
]}

Matsumoto, M ^{[1
]}

Ohnishi, S ^{[1
]}

Mochizuki, H ^{[1
]}

机构：

[1] Mochida Pharmaceut Co Ltd, Discovery Res Ctr, Shizuoka 4128524, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2004年 / 52卷 / 04期

关键词：

factor Xa inhibitor; 1-arylsulfonyl-3-piperazinone; M55551; structure-activity relationship;

D O I：

10.1248/cpb.52.459

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Compounds containing an ethylenediamine structure in place of the piperazine ring of M55113 (1) and M55551 (2) were synthesized to investigate the effects of a piperazine moiety and evaluated for activity as factor Xa (FXa) inhibitors. Most such compounds, however, exhibited lower activity (1/10-1/100) than that of M55113 and M55551 as FXa inhibitors.

引用

页码：459 / 462

页数：4

共 14 条

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