期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 15, 页码 4377-4379出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.062
关键词
histamine H(3) receptor; SAR; pharmacophore model; naphthalene; GPCR
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.
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