title: Design, synthesis and screening of quinoline-incorporated thiadiazole as a potential anticonvulsant.
abstract: A series of quinoline-incorporated substituted thiadiazole were designed and synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ)-induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity. Among the compounds tested, 6d and 6e showed protection from seizures in both the animal models at dose level of 30 mg/kg while 7f showed protection against both models at 100 mg/kg dose level. These compounds exhibited lesser CNS depression and neurotoxicity compared with clinically effective drug.
authors: Medicinal Chemistry Division, F/o Pharmacy, Jamia Hamdard, New Delhi, India.
authors: Suresh
authors: S
authors: Kumar
authors: Darpan
authors: D
authors: Kaushik
authors: Sandhya
authors: S
authors: Bawa
authors: Suroor A
authors: SA
authors: Khan
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001522:Behavior, Animal / Q000187:drug effects; D004195:Disease Models, Animal; D015195:Drug Design; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000633:toxicity; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy / Q000517:prevention & control; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: C571414:4-chloro-N-(5-(((2-chloroquinolin-3-yl)methyl)thio)-1,3,4-thiadiazol-2-yl)benzamide; D000927:Anticonvulsants; C571413:N-(5-(((2-chloroquinolin-3-yl)methyl)thio)-1,3,4-thiadiazol-2-yl)-4-methylbenzamide; D011804:Quinolines; D013830:Thiadiazoles; D010433:Pentylenetetrazole