Synthesis and Stability in Biological Media of 1H-Imidazole-1-carboxylates of ROS203, an Antagonist of the Histamine H3 Receptor

A series of carbamate derivatives of the H3 antagonist ROS203 (1) were prepared, and their lipophilicity and steric hindrance were modulated by introducing linear or branched alkyl chains of various lengths. In vitro stability studies were conducted to evaluate how structural modulations affect the...

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Veröffentlicht in:	Chemistry & biodiversity 2008-01, Vol.5 (1), p.140-152
Hauptverfasser:	Rivara, Mirko, Vacondio, Federica, Silva, Claudia, Zuliani, Valentina, Fantini, Marco, Bordi, Fabrizio, Plazzi, Pier Vincenzo, Bertoni, Simona, Ballabeni, Vigilio, Flammini, Lisa, Barocelli, Elisabetta, Mor, Marco
Format:	Artikel
Sprache:	eng
Schlagworte:	1H-Imidazole-1-carboxylate Animals Benzothiazoles - administration & dosage Benzothiazoles - chemical synthesis Benzothiazoles - pharmacology Carbamates Carboxylic Acids - chemistry Catalysis Cattle Drug Evaluation, Preclinical Drug Stability Esterases - chemistry Histamine H3 antagonist Histamine H3 Antagonists - administration & dosage Histamine H3 Antagonists - chemical synthesis Histamine H3 Antagonists - pharmacology Hydrogen-Ion Concentration Hydrolysis Imidazoles - administration & dosage Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology In vitro stability studies Injections, Intravenous Liver - enzymology Liver - metabolism Molecular Structure Porcine liver esterase Rats Receptors, Histamine H3 - drug effects ROS203 Serum Albumin, Bovine - chemistry Stereoisomerism Structure-Activity Relationship Swine
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