Synthesis and anticonvulsant activity of 4-oxo and 4-thioxo-8-bromobenzopyran derivatives.
Several thiosemicarbazones (7 and 8), 1,3-thiazolidin-4-ones (9, 10, 13, 14) and 2-thioxo-1,3-imidazolidin-4-ones (11) have been prepared starting from 8-bromo-7-hydroxy-5-methoxy-2-methyl-4-oxo-4H-1-benzopyran-6-carbaldehyde (3) and its 4-thio analogue (4). The anticonvulsant activity of all of the synthesized compounds was evaluated against maximal electrical shock (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizures. The neurotoxicity was assessed using the rota-rod test. Some of the tested compounds displayed potent anticonvulsant activity in the scPTZ test.
Ragab
Fatma Abd El-Fattah
FA
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Hassan
Ghaneya Sayed
GS
Abu Yossef
Hanan Al-Sayed
HA
Yahya
Tawfeek Ahmed Ali
TA
Abd El-Latif
Hekma A
HA
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology*; D004597:Electroshock; D007202:Indicators and Reagents; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009422:Nervous System Diseases / Q000139:chemically induced / Q000523:psychology; D010433:Pentylenetetrazole; D010672:Phenytoin / Q000494:pharmacology; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014635:Valproic Acid / Q000494:pharmacology
D000927:Anticonvulsants; D001578:Benzopyrans; D007202:Indicators and Reagents; D014635:Valproic Acid; D010672:Phenytoin; D010433:Pentylenetetrazole