Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1

被引：19

作者：

Dhanak, D ^{[1
]}

Christmann, LT ^{[1
]}

Darcy, MG ^{[1
]}

Jurewicz, AJ ^{[1
]}

Keenan, RM ^{[1
]}

Lee, J ^{[1
]}

Sarau, HM ^{[1
]}

Widdowson, KL ^{[1
]}

White, JR ^{[1
]}

机构：

[1] SmithKline Beecham Pharmaceut, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(01)00248-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery of a series of phenylalanine derived CCR3 antagonists is reported. Parallel, solution-phase library synthesis has been utilized to delineate the structure-activity relationship leading to the synthesis of highly potent, CCR3-selective antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1441 / 1444

页数：4

共 25 条

[1]

[Anonymous], ANGEW CHEM

[2] Eotasin: A VIC (very important chemokine) of allergic inflammation? [J].

Baggiolini, M .

JOURNAL OF CLINICAL INVESTIGATION, 1996, 97 (03) :587-587

[3] Human chemokines: An update [J].

Baggiolini, M ;

Dewald, B ;

Moser, B .

ANNUAL REVIEW OF IMMUNOLOGY, 1997, 15 :675-705

[4] Cloning, in vitro expression, and functional characterization of a novel human CC chemokine of the monocyte chemotactic protein (MCP) family (MCP-4) that binds and signals through the CC chemokine receptor 2B [J].

Berkhout, TA ;

Sarau, HM ;

Moores, K ;

White, JR ;

Elshourbagy, N ;

Appelbaum, E ;

Reape, TJ ;

Brawner, M ;

Makwana, J ;

Foley, JJ ;

Schmidt, DB ;

Imburgia, C ;

McNulty, D ;

Matthews, J ;

ODonnell, K ;

OShannessy, D ;

Scott, M ;

Groot, PHE ;

Macphee, C .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1997, 272 (26) :16404-16413

[5] CCR3 blockade as a new therapy for asthma [J].

Bertrand, CP ;

Ponath, PD .

EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2000, 9 (01) :43-52

[6]

Bodanszky M., 1994, The Practice of Peptide Synthesis, V2nd

[7] The chemokine/chemokine-receptor family: potential and progress for therapeutic intervention [J].

Cascieri, MA ;

Springer, MS .

CURRENT OPINION IN CHEMICAL BIOLOGY, 2000, 4 (04) :420-427

[8] Cloning, expression, and characterization of the human eosinophil eotaxin receptor [J].

Daugherty, BL ;

Siciliano, SJ ;

DeMartino, JA ;

Malkowitz, L ;

Sirotina, A ;

Springer, MS .

JOURNAL OF EXPERIMENTAL MEDICINE, 1996, 183 (05) :2349-2354

[9] Eosinophil recruitment to the lung in a murine model of allergic inflammation - The role of T cells, chemokines, and adhesion receptors [J].

Gonzalo, JA ;

Lloyd, CM ;

Kremer, L ;

Finger, E ;

Martinez, C ;

Siegelman, MH ;

Cybulsky, M ;

GutierrezRamos, JC .

JOURNAL OF CLINICAL INVESTIGATION, 1996, 98 (10) :2332-2345

[10] Chemokine receptor usage by human eosinophils - The importance of CCR3 demonstrated using an antagonistic monoclonal antibody [J].

Heath, H ;

Qin, SX ;

Rao, P ;

Wu, LJ ;

LaRosa, G ;

Kassam, N ;

Ponath, PD ;

Mackay, CR .

JOURNAL OF CLINICAL INVESTIGATION, 1997, 99 (02) :178-184

← 1 2 3 →