Arylimino-1,2,4-thiadiazolidinones: a new family of potassium channel openers.
A series of arylimino-1,2,4-thiadiazolidines were prepared using an efficient synthesis starting from thiadiazolopyridinium chlorides. All the compounds showed smooth muscular relaxant properties in rat portal veins. The different behaviour under highly depolarized conditions and the reduction of the biological effect by glyburide suggests that the arylimino-1,2,4-thiadiazolidin-3-ones may act, at least in part, via K+-induced hyperpolarization of vascular smooth cells.
Martínez
A
A
Instituto de Química Médica (CSIC), Madrid, Spain.
Castro
A
A
Cardelús
I
I
Llenas
J
J
Palacios
J M
JM
D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D015394:Molecular Structure; D009126:Muscle Relaxation / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D011169:Portal Vein / Q000187:drug effects / Q000502:physiology; D015221:Potassium Channels / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D015221:Potassium Channels; D013830:Thiadiazoles