Novel ligands for the human histamine H 1 receptor: Synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1, 2, …

…, JA Legere, A Golbraikh, A Tropsha, RG Booth

Index: Ghoneim, Ola M.; Legere, Jacqueline A.; Golbraikh, Alexander; Tropsha, Alexander; Booth, Raymond G. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 19 p. 6640 - 6658

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Citation Number: 24

Abstract

This paper reports the synthesis of a novel series of (±)-2-dimethylamino-5-and 6-phenyl-1, 2, 3, 4-tetrahydronaphthalene derivatives (5-and 6-APTs), and, corresponding affinity, functional activity, and, molecular modeling studies with regard to drug design targeting the human histamine H1 receptor. The 5-APTs have 2-to 4-fold higher H1 receptor affinity than the endogenous agonist histamine. The chemical nature of a meta-substituent on the 5- ...