Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides.
A series of substituted benzenedisulfonamide carbonic anhydrase inhibitors is described and their anticonvulsant activities are listed. One compound, 4-(4-methoxypiperidinosulfonyl)-2-chlorobenzenesulfonamide (19, UK-12130), was found to have anticonvulsant activity in animals at a dose level that gave only a minimal diuretic effect. 19 selectively increased cerebral blood flow in animals and man without producing an unacceptable level of metabolic acidosis.
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis; D001921:Brain / Q000098:blood supply / Q000187:drug effects / Q000201:enzymology; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D002415:Cats; D002560:Cerebrovascular Circulation / Q000187:drug effects*; D004232:Diuretics / Q000138:chemical synthesis; D004285:Dogs; D004597:Electroshock; D008297:Male; D051379:Mice; D051381:Rats; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014664:Vasodilation; D014665:Vasodilator Agents / Q000138:chemical synthesis*
D000927:Anticonvulsants; D002257:Carbonic Anhydrase Inhibitors; D004232:Diuretics; D013449:Sulfonamides; D014665:Vasodilator Agents