Synthesis and vasodilator effects of 3- and 7-sulfonylurea-1,2,4-benzothiadiazin-1,1-dioxides on rat aorta.
A series of substituted-1,2,4-benzothiadiazin-1,1-dioxide derivatives was designed and synthesized as potassium channel modulators. Various sulfonylurea moieties were introduced on positions 3 and 7 of the heterocycle without, or by means of, methylene and phenyl spacers. On rat aortic rings, several compounds displayed vasodilating activities, especially compound 24, which was more active than cromakalim and diazoxide at low doses (0.1 microM) and more active than diazoxide between 1 and 10 microM.
Khelili
S
S
Groupe de Pharmacochimie Moléculaire, Université Joseph Fourier, UFR de Pharmacie, Meylan, France.
Leclerc
G
G
Faury
G
G
Verdetti
J
J
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D001581:Benzothiadiazines / Q000737:chemistry / Q000494:pharmacology*; D003981:Diazoxide / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D013329:Structure-Activity Relationship; D013453:Sulfonylurea Compounds / Q000737:chemistry / Q000494:pharmacology*; D014665:Vasodilator Agents / Q000737:chemistry / Q000494:pharmacology*
D001581:Benzothiadiazines; D013453:Sulfonylurea Compounds; D014665:Vasodilator Agents; D003981:Diazoxide