Synthesis and anticonvulsant activity of certain substituted furochromone, benzofuran and flavone derivatives.
Synthesis of furochromone, 2-phenylchromone (flavone) and benzofuran derivatives substituted with thiosemicarbazide or thiazolidin-4-one moieties were accomplished. All the newly synthesized compounds were tested for their anticonvulsant activity in both subcutaneous pentylenetetrazole induced seizures (scPTZ) and maximal electric shock induced seizures (MES) tests using valproic acid and phenytoin respectively as reference standards. The most active compounds in scPTZ model were 1c, 2b, 5a and 7e showing 100% protection at 300 mg/kg upon intraperitoneal administration. Also, the effect of pre-treatment of three of the most active compounds (1c, 2b, 5a) on 4-amino pyridine-induced lethality in mice was investigated. Pre-treatment with these compounds significantly increased the latency for clonic and tonic seizures and prevented 4-amino pyridine induced death. Hence, this provides evidence for anticonvulsant activity of these compounds, and a neuroprotective activity for them. The structure-activity relationship was studied based on the obtained data.
Ragab
Fatma Abdel-Fattah
FA
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
El-Sayed
Nehad Aboul Magd
NA
Eissa
Amal Abdel Haleem Mohamed
AA
El Kerdawy
Ahmed Mahmoud
AM
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D004597:Electroshock; D005260:Female; D047309:Flavones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D008297:Male; D051379:Mice; D015394:Molecular Structure; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy* / Q000517:prevention & control; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D001572:Benzofurans; D002867:Chromones; D047309:Flavones