Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists

被引：14
|
作者：
Roche, Olivier [1 ]
Nettekoven, Matthias [1 ]
Vifian, Walter [1 ]
Sarmiento, Rosa Maria Rodriguez [1 ]
机构：
[1] F Hoffmann La Roche Ltd, Pharmaceut Res Basel, Discovery Chem, CH-4070 Basel, Switzerland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 15期
关键词：
histamine H(3) receptor; SAR; pharmacophore model; naphthalene; GPCR;
D O I：
10.1016/j.bmcl.2008.06.062
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The refinement of our original five point pharmacophore model for the H(3) receptor with the addition of a new acceptor feature is presented. The importance of this new acceptor feature for the binding and the selectivity against H(1), H(2) and H(4) has been validated using a newly synthesized naphthalene series. With the SAR deduced from several hundred naphthalene derivatives in various sub-classes the specific role of each pharmacophoric feature, by varying the geometry, size and charge of the molecules, was elucidated. This led to the discovery of a highly potent and selective new compounds series. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4377 / 4379
页数：3
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