1,2,4-Triazole Derivatives as Potential Scaffold for Anticonvulsant Activity

Abstract

The search for new anticonvulsant agent with more selectivity and lower toxicity continues to be an area of rigorous investigation in medicinal chemistry. Epilepsy is a chronic disorder of brain whose treatment consists of controlling seizures with antiepileptic drugs that very often related with side-effects which in rare circumstances can be potentially life-threatening. Triazolam and Alprazolam are established drugs used in epilepsy which have triazole moiety. The potency and broad spectrum of the pharmacological response of triazole moiety as anticonvulsant agent have attracted the attention of medicinal chemists to explore this framework for its potential. The literature shows that different substitution on triazole ring exhibit potent antiepileptic activity with no or lesser neurotoxicity. The present review is a sincere attempt to compile the reported potent triazole derivatives with significant anticonvulsant action.

Synthesis of 1,2,4-triazole derivatives and evaluation of their antioxidant activity

“…Phenolic and polyhydroxy derivatives as gallocatechin (I), epigallocatechin (II) and caffeic acid (III) (Figure 1) also were originated to illustrate a variety of useful properties such as radical scavenging [5], antiviral [6], antioxidant [7], anti-inflammatory [8], antiartherosclerotic activity [9], anticancer [10] and strong topoisomerase inhibiting activities [11]. During the last few decades, a considerable attention has been devoted to 1,2,4-triazole derivatives due to their wide spectrum of biological activities such as anticonvulsant [12], anticancer [13], antidepressant [14], antibacterial [15], antifungal [16], anti-inflammatory, analgesic [17] and antiviral activities [18]. Previously synthetic 1,2,4triazole derivatives were found to exhibit important antioxidant activity (compounds IV, V and VI) ( Figure 2) [19][20][21].…”

Synthesis and Biological Activities of Ethyl 2-(2-pyridylacetate) Derivatives Containing Thiourea, 1,2,4-triazole, Thiadiazole and Oxadiazole Moieties

“…Derivatives containing the 1,2,4-triazole core are still intensively studied as they possess potent antifungal properties [ 2 ]. Recently, 1,2,4-triazole-based compounds were reported as potential anticonvulsant [ 3 , 4 , 5 , 6 , 7 ] and anti-HIV agents [ 8 , 9 ]. Among the thiadiazole derivatives, those synthesized using the 1,3,4-thiadiazole motif were found to have number of biological activities such as anticonvulsant [ 10 , 11 ], antihypertensive [ 12 , 13 ], local anesthetic [ 14 ], anticancer [ 15 , 16 ], anti-HIV [ 17 ], anti-inflammatory [ 18 , 19 ], and hypoglycemic activities [ 20 ].…”

Synthesis and evaluation of antibacterial and antioxidant activity of novel 2-phenyl-quinoline analogs derivatized at position 4 with aromatically substituted 4H-1,2,4-triazoles

“…They possess broad spectrum of activities against most of the yeasts and filamentous fungi 2 . Among azoles, 1H-1,2,4-triazole derivatives are considered to be more interesting as they possess important pharmacological activities such as antifungal 3,4 , antiviral 5 , antioxidant [6][7][8] , antiasthmatic 9 , anticonvulsant 10 , antidepressant 11 , antithyroid 12 , anti-HIV 13 , anti-inflammatory 14 and anticancer [15][16][17] .…”