Synthesis and evaluation of anticonvulsant activity of (Z)-4-(2-oxoindolin-3-ylideneamino)-N-phenylbenzamide derivatives in mice

Autor:	Aref Moradi, Alireza Aliabadi, Marzieh Rahmani Khajouei, Ahmad Mohammadi-Farani
Jazyk:	angličtina
Rok vydání:	2018
Předmět:	Isatin medicine.medical_treatment Imine PTZ 010402 general chemistry 01 natural sciences chemistry.chemical_compound Synthesis Aniline Pharmacy and materia medica Convulsion medicine Anticonvulsant General Pharmacology Toxicology and Pharmaceutics synthesis isatin anticonvulsant ptz mes 010405 organic chemistry Antiepileptic Agents Neurotoxicity medicine.disease Combinatorial chemistry 0104 chemical sciences RS1-441 Maximal electroshock chemistry MES Original Article medicine.symptom
Zdroj:	Research in Pharmaceutical Sciences Research in Pharmaceutical Sciences, Vol 13, Iss 3, Pp 262-272 (2018)
ISSN:	1735-9414 1735-5362
Popis:	Due to resistance of some epileptic patients to the current medications and the general incidence of severe side effects of these drugs, development and discovery of novel antiepileptic drugs is crucial. Isatin-based derivatives are promising compounds as antiepileptic agents. In this study a new series of isatin-containing derivatives were synthesized via the imine formation between isatin and p-aminobenzoic acid. Subsequently, the obtained acidic compound was utilized to prepare the final amidic derivatives (4a-4l) through the reaction with various aniline derivatives. Then, their anti-seizure activity was investigated using maximal electroshock seizure (MES) as well as pentylenetetrazole (PTZ) models in mice. Neurotoxicity of target compounds was also determined by rotarod test. Tested isatin-based derivatives exhibited a favorable protection in both MES and PTZ procedures with high safety levels in neurotoxicity test. The introduced derivatives have demonstrated remarkable activity in mice and could be suggested as potential anticonvulsant lead compounds. All methoxylated derivatives (4j, 4k, 4l) showed a significant anti-seizure activity in MES model. Compounds 4j (2-OCH3) and 4l (4-OCH3) also demonstrated a potent anti-seizure activity against PTZ. Compound 4k (m-OCH3) did not induce protection towards PTZ-induced convulsion.
Databáze:	OpenAIRE
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