UNSYMMETRICALLY SUBSTITUTED GUANIDINES AS POTENT HISTAMINE H-3 RECEPTOR ANTAGONISTS

Authors
STARK H KRAUSE M ARRANG JM LIGNEAU X SCHWARTZ JC SCHUNACK W
Citation
H. Stark et al., UNSYMMETRICALLY SUBSTITUTED GUANIDINES AS POTENT HISTAMINE H-3 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(24), 1994, pp. 2907-2912
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
24
Year of publication
1994
Pages
2907 - 2912
Database
ISI
SICI code
0960-894X(1994)4:24<2907:USGAPH>2.0.ZU;2-P
Abstract
Unsymmetrically trisubstituted and disubstituted guanidine derivatives of (1H-imidazol-4-yl)alkyl amines were synthesized and investigated f or histamine H-3-receptor activity. Electron-withdrawing substitution of the guanidino group resulted in antagonists with a potential prodru g character. The H-3-receptor selective -cyclohexylmethyl-N-2-[3-(1H-i midazol-4-yl)propyl] guanidine possesses a -log K-i of 9.1.