Synthesis, physicochemical and anticonvulsant properties of new N-pyridyl derivatives of 3-phenyl- and 3,3-diphenyl-succinimides.
Synthesis and physicochemical properties of new N-pyridyl derivatives of 3-phenyl and 3,3-diphenylsuccinimides (1-12) have been described. The obtained compounds were evaluated in respect of their anticonvulsant activity. The N-pyridyl derivatives of 3-phenylsuccinimides (7-12) abolished the protection against MES- and scMET-induced seizures, whereas N-pyridyl derivatives of 3,3-diphenylsuccinimides (1-6) were inactive. After molecular modelling and quantum-chemistry calculations the theoretical activity test was applied (W. Kwiatkowski, J. Karolak-Wojciechowska, SAR and QSAR Envir. Res. 1 (1993) 233; Chem. Abstr. 120, 153001 (1994). J. Karolak-Wojciechowska, M. Blaszczyk, W. Kwiatkowski, J. Obniska, A. Zejc, J. Chem. Cryst. 27 (1997) 297; Chem. Abstr. 127, 277834k (1997)). The molecular electrostatic potential (MEP) of the active compounds differed significantly from that of the inactive ones.
Obniska
J
J
Department of Medicinal Chemistry, Collegium Medicum of Jagiellonian University, Krakow, Poland.
Zejc
A
A
Karolak-Wojciechowska
J
J
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004597:Electroshock; D008968:Molecular Conformation; D010433:Pentylenetetrazole; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013056:Spectrophotometry, Ultraviolet; D013388:Succinimides / Q000138:chemical synthesis* / Q000494:pharmacology; D014961:X-Ray Diffraction
D000927:Anticonvulsants; D011725:Pyridines; D013388:Succinimides; D010433:Pentylenetetrazole