Synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives potassium channel openers.
As part of a search for new potassium channel openers, the synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives derived from transformation of the benzopyran skeleton of cromakalim were described. Several new 1,4-benzoxazine derivatives were provided with significant vasorelaxant activity with an overall pharmacological behavior similar to CRK (1f, 1i, 2d, 2e, 2f and 2i).
Caliendo
Giuseppe
G
Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy. caliendo@unina.it
Perissutti
Elisa
E
Santagada
Vincenzo
V
Fiorino
Ferdinando
F
Severino
Beatrice
B
di Villa Bianca
Roberta d'Emmanuele
Rd
Lippolis
Laura
L
Pinto
Aldo
A
Sorrentino
Raffaella
R
D000818:Animals; D001011:Aorta / Q000187:drug effects; D019806:Cromakalim; D004305:Dose-Response Relationship, Drug; D015640:Ion Channel Gating / Q000187:drug effects; D008297:Male; D010078:Oxazines / Q000138:chemical synthesis* / Q000494:pharmacology; D015221:Potassium Channels / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014664:Vasodilation / Q000187:drug effects*
D010078:Oxazines; D015221:Potassium Channels; D019806:Cromakalim