N-ALPHA-ALKYLATED DERIVATIVES OF 2-PHENYLHISTAMINES - SYNTHESIS AND IN-VITRO ACTIVITY OF POTENT HISTAMINE H-1-RECEPTOR AGONISTS

Authors
KRAMER K ELZ S PERTZ HH SCHUNACK W
Citation
K. Kramer et al., N-ALPHA-ALKYLATED DERIVATIVES OF 2-PHENYLHISTAMINES - SYNTHESIS AND IN-VITRO ACTIVITY OF POTENT HISTAMINE H-1-RECEPTOR AGONISTS, Bioorganic & medicinal chemistry letters, 8(18), 1998, pp. 2583-2588
Citations number
28
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
18
Year of publication
1998
Pages
2583 - 2588
Database
ISI
SICI code
0960-894X(1998)8:18<2583:NDO2-S>2.0.ZU;2-E
Abstract
New potent N-alpha-alkylated histamine HI-receptor agonists have been prepared and functionally evaluated for partial agonist potency and se lectivity. -alpha-Methyl-2-(3-trifluoromethylphenyl)histamine contract s ileal segments and aortic rings of guinea-pig with a relative potenc y of 174% (95% confid. lim. 161 - 188%) and 217% (164 - 287%), respect ively (histamine: 100%) and is the most potent H-1 receptor agonist de scribed so far. (C) 1998 Elsevier Science Ltd. All rights reserved.