ChemInform Abstract: Synthesis of Potent Non‐Imidazole Histamine H₃‐Receptor Antagonists.

Abstract

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Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies

“…[18] The potential liability of imidazole-containing compounds with respect to cytochrome P450 inhibition and drug-drug interactions led to the development of potent and selective non-imidazole derivatives, including compounds such as ABT-239 1, UCL 1972 2, JNJ-5207852 3, GSK-189254 4, Novo Nordisk's 5 and Merck's 6 ( Figure 1). [19][20][21][22][23] These intense efforts made by numerous pharmaceutical companies led to the development of a new refined H 3 antagonist pharmacophore model which contains three parts: a basic amine moiety (western part) able to interact with ASP3.32, an amino acid of the receptor [24], linked via a variable alkyl spacer to a central core, and an additional eastern part displaying a high chemical diversity ( Fig. 1).…”