157847-53-5Relevant articles and documents
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents
Carson, John R.,Carmosin, Richard J.,Pitis, Philip M.,Vaught, Jeffry L.,Almond, Harold R.,Stables, James P.,Wolf, Harold H.,Swinyard, Ewart A.,White, H. Steve
, p. 1578 - 1584 (1997)
2-Aroyl-4-(ω-aminoacyl)- (4) and 4-aroyl-2-(ω-aminoacyl)pyrroles (9) represent a new, structurally novel class of anticonvulsant agents. Compounds of type 4 were prepared by Friedel-Crafts acylation of a 2-aroylpyrrole with an ω-chloroacyl chloride followed by displacement of the chloro group by a primary or secondary amine. Compounds of type 9 were prepared by Friedel- Crafts aroylation of a 2-(ω-chloroacyl)pyrrole followed by displacement by an amine. These compounds were active in the mouse and rat maximal electroshock tests but not in the mouse metrazole test. The lead compound, RWJ-37868, 2-(4-chlorobenzoyl)-4-(1-piperidinyl-acetyl)-1,3,5- trimethylpyrrole (4d), showed potency and therapeutic index comparable to those of phenytoin and carbamazepine and greater than those of sodium valproate. This compound blocked bicuculline induced seizures, did not elevate seizure threshold following iv infusion of metrazole, and blocked influx of Ca2+ ions into cerebellar granule cells induced by K+ or veratridine.
Aroyl aminoacyl pyrroles for use in the treatment of neuropathic pain
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, (2008/06/13)
Aroyl aminoacyl pyrroles are pharmaceutically useful in treating neuropathic pain, which includes utility for the treatment of neuropathic pain.
