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Synthesis, SAR and selectivity of 2-acyl- and 2-cyano-1-hetarylalkyl-guanidines at the four histamine receptor subtypes: a bioisosteric approach

Geyer, Roland ; Igel, Patrick ; Kaske, Melanie ; Elz, Sigurd ; Buschauer, Armin


In 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 H1,2,3,4Rs, isolated guinea-pig organs (H1R, ...


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