Recent progress of 1,3,4‐oxadiazoles as anticonvulsants: Future horizons

Abstract

Epilepsy is the most common neurological disorder, which affects more than 50 million people worldwide. Despite the development and use of several antiepileptic drugs (AEDs), attempted seizure control fails in almost 30% of the individuals treated. Other patients benefit from seizure control by drug therapy at the expense of dose‐related toxicity and side effects. These drawbacks with conventional AEDs demand the need for developing more effective and safer antiseizure agents. As a result, extensive efforts are devoted to design and develop new effective molecules as antiepileptics. This area of research to find more effective and safer AEDs is important and challenging. This review describes the future perspective of various 1,3,4‐oxadiazole derivatives as anticonvulsant agents and focuses on the design and development of the new effective molecule.

Synthesis of Novel Triazolyl/Oxadiazolyl/Thiadiazolyl-Piperazine as Potential Anticonvulsant Agents

“…The newly synthesized compounds i. e. compounds (3-8), (9)(10)(11)(12)(13)(14), (15)(16)(17)(18)(19)(20) and (21)(22)(23)(24)(25)(26) were studied for anticonvulsant activity at a dose of 30 mg/kg i.p. These compounds were also evaluated for approximate lethal dose (ALD 50 ).…”

“…Further, the series was characterized by its trifurcation which leads to the synthesis of triazoles (9)(10)(11)(12)(13)(14), oxadiazole (15)(16)(17)(18)(19)(20) and thiadiazoles (21)(22)(23)(24)(25)(26). Studying the anticonvulsant activity of triazoles (9)(10)(11)(12)(13)(14) it was noticed that compound 9 having substitution with bromo group at 2 nd position of phenyl ring showed good protection of 80 % against seizures which is equipotent to standard drug phenytoin sodiyum (80 %).…”

“…Compounds (15)(16)(17)(18)(19)(20) having different substituted oxadiazole moiety on phenyl piperazine have shown varying degree (50-80 %) of anticonvulsant activity. However, the effect of different substitutions was found to be similar with that of compounds (9)(10)(11)(12)(13)(14).…”

“…Moreover, various versatile pharmacophores such as triazoles [11][12][13][14], oxadiazoles [15][16][17][18][19] and thiadiazoles [20][21][22] possess anticonvulsant activity. Several scientists have also elucidated that the modifications at 1 st or 4 th position in piperazine nucleus by different heterocyclic moieties yielded potent anticonvulsant agents.…”

Ultrasound-Assisted Synthesis, Antioxidant Activity and Computational Study of 1,3,4-Oxadiazol-2-amines

“…10 1,3,4-Oxadiazole derivatives have attracted a great deal of interest due to their diverse biological properties Beyzaei et al: Ultrasound-Assisted Synthesis, Antioxidant Activity ... such as antioxidant, antiproliferative, anticonvulsant, antimicrobial and anti-Alzheimer. [11][12][13][14][15] Synthetic approaches of 1,3,4-oxadiazoles were reviewed in several literatures. [16][17][18] Hypervalent iodine mediated reaction of N´-arylidene acetohydrazides, intracyclocondensation of thiosemicarbazides prepared from the reaction of aryl hydrazides with ammonium thiocyanate using N,N,N´,N´-tetramethyl-O-(benzotriazol-1-yl)uronium tetrafluoroborate (TBTU) or N,N´-diisopropylcarbodiimide (DIC), and simultaneous reaction of 1-chloroketones, N-isocyaniminotriphenylphosphorane and aryl carboxylic acids are examples of recent methods proposed to synthesize 1,3,4-oxadiazole derivatives.…”