title: Anticonvulsant properties of selected pyrrolo[2,3-d]pyrimidine-2,4-diones and intermediates.
abstract: A series of pyrrolo[2,3-d]pyrimidine-2,4-diones and intermediates was tested for anticonvulsant activity in mice. Eleven of the 15 compounds possessed anticonvulsant activity against pentylenetetrazol-induced convulsions. One compound afforded more anticonvulsant protection against pentylenetetrazol than did trimethadione (67 and 50%, respectively). A suspension of this compound was found to be as effective as a solution in producing anticonvulsant activity. The results suggest that the nitrile analogs were more potent compared to the carbamyl analog due to higher lipid solubility.
mesh_terms: D000818:Animals; D000927:Anticonvulsants; D004597:Electroshock; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole; D010672:Phenytoin / Q000494:pharmacology; D011744:Pyrimidinones / Q000008:administration & dosage / Q000494:pharmacology*; D011758:Pyrroles / Q000008:administration & dosage / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D012995:Solubility; D013329:Structure-Activity Relationship; D014293:Trimethadione / Q000494:pharmacology
chemical_list: D000927:Anticonvulsants; D011744:Pyrimidinones; D011758:Pyrroles; D010672:Phenytoin; D014293:Trimethadione; D010433:Pentylenetetrazole