Cinnamic amides of (S)-2-(aminomethyl)pyrrolidines are potent H3 antagonists.
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.
Peschke
Bernd
B
Protein and Peptide Chemistry, Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark. bpes@novonordisk.com
Bak
Sonja
S
Hohlweg
Rolf
R
Pettersson
Ingrid
I
Refsgaard
Hanne Hoffmann Frølund
HH
Viuff
Dorthe
D
Rimvall
Karin
K
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
D000577:Amides; D002934:Cinnamates; D065607:Cytochrome P-450 Enzyme Inhibitors; D006633:Histamine Antagonists; D011759:Pyrrolidines; D016244:Guanosine 5'-O-(3-Thiotriphosphate)