3-[3-(Piperidinomethyl)phenoxy]alkyl, N-cyano-N'-[omega-[3-(1-piperidinylmethyl)phenoxy]alkyl]guanidine and 2-(5-methyl-4-imidazolyl)methyl thioethyl derivatives containing fluorescent functionalities were synthesized and the histamine H2 receptor affinity was evaluated using the H2 antagonist [125I]-aminopotentidine. The compounds exhibited weak to potent H2 receptor affinity with pKi values ranging from <4 to 8.85. The highest H2 receptor affinity was observed for N-cyano-N'-[omega-[3-(1-piperidinylmethyl)phenoxy]alkyl]guanidines substituted with methylanthranilate (13), cyanoindolizine (6) and cyanoisoindole (11) moieties via an ethyl or propyl linker.
Fluorescent Ligands for the Histamine H2 Receptor: Synthesis and Preliminary Characterization / SAREL F., Malan; ANDRE VAN, Marle; WIRO M., Menge; Zuliani, Valentina; Marcel, Hoffman; Henk, Timmerman; Rob, Leurs. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 14:(2004), pp. 6495-6503. [10.1016/j.bmc.2004.09.018]
Fluorescent Ligands for the Histamine H2 Receptor: Synthesis and Preliminary Characterization
ZULIANI, Valentina;
2004-01-01
Abstract
3-[3-(Piperidinomethyl)phenoxy]alkyl, N-cyano-N'-[omega-[3-(1-piperidinylmethyl)phenoxy]alkyl]guanidine and 2-(5-methyl-4-imidazolyl)methyl thioethyl derivatives containing fluorescent functionalities were synthesized and the histamine H2 receptor affinity was evaluated using the H2 antagonist [125I]-aminopotentidine. The compounds exhibited weak to potent H2 receptor affinity with pKi values ranging from <4 to 8.85. The highest H2 receptor affinity was observed for N-cyano-N'-[omega-[3-(1-piperidinylmethyl)phenoxy]alkyl]guanidines substituted with methylanthranilate (13), cyanoindolizine (6) and cyanoisoindole (11) moieties via an ethyl or propyl linker.File | Dimensione | Formato | |
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