Benzothiazole incorporated barbituric acid derivatives: synthesis and anticonvulsant screening.
A series of 1-(6-substituted-1,3-benzothiazol-2-yl)-3-(substituted phenyl)hexahydro-2,4,6-pyrimidinetriones 4a-t were synthesized starting from substituted anilines. These compounds contained two active anticonvulsant pharmacophores, benzothiazole and barbituric acid. Structures of the compounds were confirmed on the basis of different spectroscopic techniques. All the compounds were evaluated for their anticonvulsant activity. Three compounds 4c, 4d, and 4s showed promising anticonvulsant activities in Maximal Electroshock Seizure test (MES) and subcutaneous pentylenetetrazole test (scPTZ). They also displayed a wide safety profile when tested for the minimal motor impairment test.
Siddiqui
Nadeem
N
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi, India. nadeems_03@yahoo.co.in
Ahsan
Waquar
W
D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000627:therapeutic use*; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use*; D001463:Barbiturates / Q000138:chemical synthesis* / Q000627:therapeutic use*; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000627:therapeutic use*; D001665:Binding Sites; D004353:Drug Evaluation, Preclinical; D004597:Electroshock; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000814:Aniline Compounds; D000927:Anticonvulsants; D001463:Barbiturates; D052160:Benzothiazoles; C005465:benzothiazole; D010433:Pentylenetetrazole; C032232:barbituric acid