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Fluorescent ligands for the histamine H2 receptor: synthesis and preliminary characterization |
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| Authors: | Malan Sarel F van Marle Andre Menge Wiro M Zuliani Valentina Zuliana Valentina Hoffman Marcel Timmerman Henk Leurs Rob |
| Institution: | aPharmaceutical Chemistry, North-West University, Potchefstroom 2520, South Africa bLeiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, Amsterdam, The Netherlands |
| Abstract: | 3-3-(Piperidinomethyl)phenoxy]alkyl, N-cyano-N′-ω-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′-ω-3-(1-piperidinylmethyl)phenoxy]alkyl]guanidines substituted with methylanthranilate (13), cyanoindolizine (6) and cyanoisoindole (11) moieties via an ethyl or propyl linker. |
| Keywords: | Fluorescent histamine H2 ligands |
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