NOVEL H-3 RECEPTOR ANTAGONISTS - SULFONAMIDE HOMOLOGS OF HISTAMINE

Authors
WOLIN R CONNOLLY M AFONSO A HEY JA SHE H RIVELLI MA WILLAMS SM WEST RE
Citation
R. Wolin et al., NOVEL H-3 RECEPTOR ANTAGONISTS - SULFONAMIDE HOMOLOGS OF HISTAMINE, Bioorganic & medicinal chemistry letters, 8(16), 1998, pp. 2157-2162
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
16
Year of publication
1998
Pages
2157 - 2162
Database
ISI
SICI code
0960-894X(1998)8:16<2157:NHRA-S>2.0.ZU;2-R
Abstract
Sulfonamides derived from 4(5)-(omega-aminoalkyl)-1H-imidazoles contai ning chain lengths of three- to five-carbons were synthesized. Good to moderate H-3 receptor binding affinities were observed for several bu tyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series. Separation of the imidazole ring and the sulfonamide unit by a four- or five-carbon tether afforded potent H-3 receptor antagonists. (C) 1998 Elsevier Science Ltd. All rights reserv ed.