Anticonvulsant and neurotoxicity evaluation of new bromophthalimidobutyryl amide derivatives.
A series of 4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-butyryl N-(substituted phenyl) amides (3a-I) were synthesized and evaluated for their anticonvulsant activity in MES test according to the protocols of Antiepileptic Drug Development (ADD) programme of National Institutes of Health (NIH, Bethesda, USA).The most active compounds of the series were 3a, 3c, 3d, 3f, 3g, 3i and 3k at the dose of 30 mg/kg (i.p.) 0.5 h and 4 h after administration. In neurotoxic screen (NT), 3d, 3i and 3k were less toxic when compared with the other compounds.
Khan
Suroor A
SA
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.
Siddiqui
Nadeem
N
Kamal
Mehnaz
M
Alam
Ozair
O
Jawaid
Talha
T
D000577:Amides / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000633:toxicity; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D004597:Electroshock; D051379:Mice; D009316:National Institutes of Health (U.S.); D020258:Neurotoxicity Syndromes / Q000209:etiology; D012640:Seizures / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013997:Time Factors; D018675:Toxicity Tests; D014481:United States
D000577:Amides; D000927:Anticonvulsants