Zusammenfassung
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e. g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine- type H4R agonists (e. g. UR-PI376), the contribution of various heterocycles to agonism, antagonism and HR subtype selectivity was studied (recombinant human H(1,2,3,4)Rs, isolated guinea pig ...
Zusammenfassung
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e. g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine- type H4R agonists (e. g. UR-PI376), the contribution of various heterocycles to agonism, antagonism and HR subtype selectivity was studied (recombinant human H(1,2,3,4)Rs, isolated guinea pig organs (H1R, H2R)). While minor structural modifications of UR- PI376 analogues were not tolerated regarding H4R agonism, in the case of the acylguanidines, a 1,2,4-triazole ring shifted the selectivity toward the H2R.
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