Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles

被引：17

作者：

Nishizawa, Rena ^{[1
]}

Nishiyama, Toshihiko ^{[1
]}

Hisaichi, Katsuya ^{[1
]}

Hirai, Keisuke ^{[1
]}

Habashita, Hiromu ^{[1
]}

Takaoka, Yoshikazu ^{[3
]}

Tada, Hideaki ^{[2
]}

Sagawa, Kenji ^{[4
]}

Shibayama, Shiro ^{[2
]}

Maeda, Kenji ^{[5
,6
]}

Mitsuya, Hiroaki ^{[5
,6
]}

Nakai, Hisao ^{[1
]}

Fukushima, Daikichi ^{[1
]}

Toda, Masaaki ^{[1
]}

机构：

[1] Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan

[2] Ono Pharmaceut Co Ltd, Tsukuba Res Inst, Ibaraki 300424, Japan

[3] Ono Pharmaceut Co Ltd, Fukui Res Inst, Fukui 9138538, Japan

[4] Ono Pharmaceut Co Ltd, Osaka 5410056, Japan

[5] Kumamoto Univ, Sch Med, Dept Internal Med 2, Kumamoto 8600811, Japan

[6] NCI, Expt Retrovirol Sect, HIV & AIDS Malignancy Branch, NIH, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 02期

关键词：

CCR5; Chemokine; Anti HIV-1; HIV-1; ENTRY; CORECEPTOR; COFACTOR; RECEPTOR; POTENT;

D O I：

10.1016/j.bmcl.2009.11.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：763 / 766

页数：4

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