Abstract
On the basis of the suggestions provided by our previous studies concerning the antagonistic activity detected for two series of thioperamide analogues at ileal histamine H3-heteroreceptors, here we describe the data obtained for newly synthesized imidazole derivatives tested in the same functional model. Such molecules were designed by replacing the non-imidazolyl portion of the previously studied H3-blocker ***1-(benzothiazol-2-yl)-4-[(1H)-imidazol-4-yl]piperidine with more flexible and less bulky moieties. The structural manipulations of this chemical starting point involved the replacement of piperidine moiety with ethylaminic or ethylthio chain and the exchange of benzothiazole nucleus with benzimidazole or with phenyl substituted or unsubstituted thiazole/imidazole ring. By testing such substances on guinea-pig isolated preparations suitable for functional assessment of their affinity at histamine receptor subtypes, we selected the compound ***1-[4(5)-phenyl-(2-imidazolylthio)]-2-[4(5)-imidazolyl]etan (cVII) as a lead molecule for further investigations on such structure-activity relationships.
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