title: Cinnamic amides of (S)-2-(aminomethyl)pyrrolidines are potent H3 antagonists.
abstract: New imidazole-free H3 antagonists have been found in a series of cinnamic amides of (S)-(aminomethyl)pyrrolidines. The influence of the substituent on the aromatic moiety on the potency and the inhibition of three cytochrome P450 subtypes are also described.
authors.affiliation: Protein and Peptide Chemistry, Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark. bpes@novonordisk.com
authors.forename: Bernd
authors.initials: B
authors.lastname: Peschke
authors.forename: Sonja
authors.initials: S
authors.lastname: Bak
authors.forename: Rolf
authors.initials: R
authors.lastname: Hohlweg
authors.forename: Ingrid
authors.initials: I
authors.lastname: Pettersson
authors.forename: Hanne Hoffmann Frølund
authors.initials: HH
authors.lastname: Refsgaard
authors.forename: Dorthe
authors.initials: D
authors.lastname: Viuff
authors.forename: Karin
authors.initials: K
authors.lastname: Rimvall
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D016466:CHO Cells; D002934:Cinnamates / Q000737:chemistry* / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D065607:Cytochrome P-450 Enzyme Inhibitors; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D011759:Pyrrolidines / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000577:Amides; D002934:Cinnamates; D065607:Cytochrome P-450 Enzyme Inhibitors; D006633:Histamine Antagonists; D011759:Pyrrolidines; D016244:Guanosine 5'-O-(3-Thiotriphosphate)