Hit-to-lead studies: The discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists

被引:47
作者
Baxter, A [1 ]
Bennion, C [1 ]
Bent, J [1 ]
Boden, K [1 ]
Brough, S [1 ]
Cooper, A [1 ]
Kinchin, E [1 ]
Kindon, N [1 ]
McInally, T [1 ]
Mortimore, M [1 ]
Roberts, B [1 ]
Unitt, J [1 ]
机构
[1] AstraZeneca R&D Charnwood, Loughborough LE11 5RH, Leics, England
关键词
D O I
10.1016/S0960-894X(03)00561-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A Hit-to-Lead optimisation programme was carried out on the high throughput screening hit, the triazolethiol 1, resulting in the discovery of the potent, orally bioavailable triazolethiol CXCR2 receptor antagonist 45. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2625 / 2628
页数:4
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