Design and synthesis of anticonvulsants from a combined phthalimide-GABA-anilide and hydrazone pharmacophore.
Two series of pharmacophoric hybrids of phthalimide-GABA-anilides/hydrazones were designed and synthesized and evaluated for their anticonvulsant and neurotoxic properties. The structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. Initial anticonvulsant screening was performed using intraperitoneal (i.p.) maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and intraperitoneal picrotoxin (ipPIC)-induced seizure threshold tests. All of the compounds were ineffective in the MES test. Most of the compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model.
Ragavendran
Jegadeesan Vaigunda
JV
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Vidya Vihar, Pilani, Rajasthan 333031, India.
Sriram
Dharmarajan
D
Patel
Sravan Kumar
SK
Reddy
Ingala Vikram
IV
Bharathwajan
Narayanan
N
Stables
James
J
Yogeeswari
Perumal
P
D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D004195:Disease Models, Animal; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D045442:Rotarod Performance Test; D012640:Seizures / Q000188:drug therapy / Q000209:etiology / Q000517:prevention & control; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
D000813:Anilides; D000927:Anticonvulsants; D006835:Hydrazones; D010797:Phthalimides; D005680:gamma-Aminobutyric Acid