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Medicinal Chemical and Pharmacological Aspects of Imidazole-Containing Histamine H3 Receptor Antagonists

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The first antagonists known for the histamine H3 receptor were mono-substituted imidazolecontaining compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.
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Keywords: cipralisant; ciproxifan; clobenpropit; h3 receptor; imidazole; radioligand; sch 79687; thioperamide

Document Type: Review Article

Affiliations: Johann Wolfgang Goethe-Universitat, Institut fur Pharmazeutische Chemie, Biozentrum, Marie- Curie-Strasse 9, 60439 Frankfurt am Main, Germany.

Publication date: November 1, 2004

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  • The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

    The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

    Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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