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

共 50 条

[21] Small Molecule Antagonists of the Chemokine Receptor CCR5
Lemoine, Remy C.
Wanner, Jutta
CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2010, 10 (13) : 1299 - 1338
[22] Isolation and structure of antagonists of chemokine receptor (CCR5)
Jayasuriya, H
Herath, KB
Ondeyka, JG
Polishook, JD
Bills, GF
Dombrowski, AW
Springer, MS
Siciliano, S
Malkowitz, L
Sanchez, M
Guan, ZQ
Tiwari, S
Stevenson, DW
Borris, RP
Singh, SB
JOURNAL OF NATURAL PRODUCTS, 2004, 67 (06): : 1036 - 1038
[23] What is the future of CCR5 antagonists in rheumatoid arthritis?
Takeuchi, Tsutomu
Kameda, Hideto
ARTHRITIS RESEARCH & THERAPY, 2012, 14 (02)
[24] Secondary effects of treatment with maraviroc and other CCR5 antagonists. Potential impact of the CCR5 blocker
Arribas Lopez, Jose R.
ENFERMEDADES INFECCIOSAS Y MICROBIOLOGIA CLINICA, 2008, 26 : 23 - 27
[25] CCR5 antagonists as anti-HIV agents
不详
DRUG DISCOVERY TODAY, 2001, 6 (14) : 747 - 747
[26] What is the future of CCR5 antagonists in rheumatoid arthritis?
Tsutomu Takeuchi
Hideto Kameda
Arthritis Research & Therapy, 14
[27] CCR5 antagonists as anti-HIV agents
Lloyd, AW
DRUG DISCOVERY TODAY, 2000, 5 (09) : 428 - 429
[28] Transgenic mouse expressing human CCR5 as a model for in vivo assessments of human selective CCR5 antagonists
Saita, Y
Kondo, M
Miyazaki, T
Yamaji, N
Shimizu, Y
EUROPEAN JOURNAL OF PHARMACOLOGY, 2005, 518 (2-3) : 227 - 233
[29] The design and discovery of novel amide CCR5 antagonists
Pryde, David C.
Corless, Martin
Fenwick, David R.
Mason, Helen J.
Stammen, Blanda C.
Stephenson, Peter T.
Ellis, David
Bachelor, David
Gordon, David
Barber, Christopher G.
Wood, Anthony
Middleton, Donald S.
Blakemore, David C.
Parsons, Gemma C.
Eastwood, Rachel
Platts, Michelle Y.
Statham, Keith
Paradowski, Kerry A.
Burt, Catherine
Klute, Wolfgang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (04) : 1084 - 1088
[30] Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO-K1 cells
Longden, J.
Cooke, E-L
Hill, S. J.
BRITISH JOURNAL OF PHARMACOLOGY, 2008, 153 (07) : 1513 - 1527

← 1 2 3 4 5 →