76813-81-5Relevant academic research and scientific papers
N-phenyl-N'-pyridinylureas as anticonvulsant agents
Pavia,Lobbestael,Taylor,Hershenson,Miskell
, p. 854 - 861 (2007/10/02)
A series of N-phenyl-N'-pyridinylureas was examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N'-(4-pyridinyl)urea series, with 37 exhibiting the best overall anticonvulsant profile. Compound 37 was effective against seizures induced by maximal electroshock but did not protect mice from clonic seizures produced by the convulsant pentylenetetrazol. The overall pharmacological profile suggests that 37 would be of therapeutic use in the treatment of generalized tonic-clonic and partial seizures. Compound 37 was selected for Phase 1 clinical trials.
5-Hydroxytryptamine (5-HT3) Receptor Antagonists. 3. Ortho-Substituted Phenylureas
Bermudez, Jose,Dabbs, Steven,King, Frank D.
, p. 1932 - 1935 (2007/10/02)
A novel series of potent 5-HT3 receptor antagonists, ortho-substituted phenylureas 6a-z, is described in which the 5-membered ring of the previously reported indazoles and indolines has been replaced by an intramolecular hydrogen bond.High potency was found both for carbamate 6a and urea 6b.Granatane 6c was less potent than the equivalent tropane.Phenylurea 11c lacking the ortho substituent was inactive.Whereas further substitution could not be tolerated in the aromatic ring, activity was retained with a range of O-alkyl groups, compounds 6k-t.In addition, good activity was found for ortho ester 6u and sulfonamide 6x.The ortho-substituted phenylureas can therefore be regarded as bioisosteres of the 6,5-heterocycles indole, indazole, and indoline.
