Histamine H 3 and H 4 receptor affinity of branched 3-(1H-imidazol-4-yl) propyl N-alkylcarbamates

…, W Schunack, H Stark, K Kieć-Kononowicz

Index: Lazewska, Dorota; Wiecek, Malgorzata; Ligneau, Xavier; Kottke, Tim; Weizel, Lilia; Seifert, Roland; Schunack, Walter; Stark, Holger; Kiec-Kononowicz, Katarzyna Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6682 - 6685

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Citation Number: 16

Abstract

A series of imidazole-containing (non-) chiral carbamates were tested at human histamine H3 receptor (H3R). All compounds displayed Ki values below 100nM. A trend for a stereoselectivity at human H3R was observed for the chiral α-branched ligands. Selected compounds were also tested at human histamine H4 receptor and showed moderate to weak affinities (118–1460nM).