Synthesis, Anticonvulsant and Neurotoxicity Screening of Some Novel 2, 5-Disubstituted - 1, 3, 4 – Oxadiazole Derivatives

Abstract

A series of 2, 5-disubstituted - 1, 3, 4 oxadiazoles (4a-o) were synthesized on refluxing hydrazine carbothioamides with iodine and potassium iodide in ethanolic sodium hydroxide solution starting from methyl-3-amino-4-hydroxy benzoate via synthesis of an intermediate methyl-2-substitutedaryl-1, 3-benzoxazole-5-carboxylates and 2-substitutedaryl-1, 3-benzoxazole-5-carbohydrazides. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, 1H-NMR, MS) and elemental analysis. All these compounds were screened for anticonvulsant activity using Maximal Electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) method. Anticonvulsant activity was shown by majority of the synthesized compounds when given i.p. to mice. Among the tested compounds 4e, 4j and 4o were considered to have potent anticonvulsant activity comparable to that of standard drugs Phenytoin and Carbamazepine. Compounds 4e, 4g, 4h, 4i, 4k and 4m passed the rota rod test successfully without any sign of neurological deficit.

Studies on New Schiff bases of Benzoxazole: Synthesis, Anticonvulsant and Neurotoxicity Evaluation

“…A mixture of 2-chloro-4-nitrobenzoic acid and methyl-3-amino-4-hydroxybenzoate (0.01mol) refluxed about 15 hours. Then reaction mixtures poured, cooled over the squashed ice by mixing for acquire the compounds 8,[27][28] .…”

“…In absolute ethanol, an equimolar quantity of a mixture of hydrazine hydrate and methyl 2-(2-chloro-4-nitrophenyl)-1,3-benzoxazole-5carboxylate was heated under the reflux (18-20 hours). Obtained complex were cooled and the found solids was filtered crystallized by using ethanol 8,[27][28] .…”

“…However, a large number of individuals with epilepsy are insensitive to current medications, and they have been experiencing a wide range of side effects [4][5] . Although new medications like pregabalin and retigabine have become available in the last decade, their efficacy remains questionable, and have only been used in some certain types of epilepsy [6][7][8] . Existing AEDs are systemic in their effect, which means they lack selectivity to one target site and as a result it causes a lot of adverse effects such as psychosis, cerebellar syndrome, gingival hyperplasia and cardiac arrhythmia [9][10] .…”

Synthesis of some new 1-(5-((1H-pyrazol-1-yl)methyl)-2-aryl-1,3,4-oxadiazol-3(2H)-yl) ethanone derivatives and study their antimicrobial activity

“…1,3,4-oxadiazole derivatives have been possessed diverse biological activities such as antimicrobial, antitubercular, antimalarial, antiviral [16][17][18], analgesic, anti-in ammatory, CNS depressant, anticonvulsant, hypnotic, sedative, muscle relaxants [19], insecticidal, herbicidal [20], antitumor, cytotoxic [21,22], lipid peroxidation inhibitor, diuretic, antioxidant [23], etc. Therefore, 1,3,4-oxadiazoles have attracted researchers all over the world to work in this area of new drug development.…”

Synthesis, Spectral Characterization and Anticonvulsant Studies of the Novel Triazolothiadiazoles Bearing Benzoxazole Moiety

“…It is the acts of abrupt qualitative and quantitative unsettling influences of consciousness, and of sensor, autonomic and motor function and is the second most predominant neurological scatter in the industrial world 3 . In worldwide battle, World Health Organization (WHO) targeting epilepsy by the organization with the International Bureau for Epilepsy (IBE) plus International League Against Epilepsy (ILAE) roughly about 0.5-1% to the general populace will be affected, whenever is harrowed with this neurological disorder 4 . Each year nearly 2.5 million new cases are added to these numbers [4][5][6][7] .…”