Abstract
A series of amidine substituted phenyl-, benzyl-, and phenethylimidazoles based on the known H 3 agonist SK&F 91606 ( 4) has been synthesized and tested as ligands for the histamine H 3 receptor. Insertion of a phenyl ring between the imidazole ring and the amidine moiety produces antagonists. The benzyl series was found to be the most potent and was further investigated. Compounds 9c and 18 (entries 5 and 12, Table 1) are potent ligands for the H 3 receptor with K i values of 16 nM and 7.2 nM respectively. In vivo, both compounds were shown to be equipotent to thioperamide ( 2), the standard H 3 antagonist.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
