Synthesis and Studies on the Anticonvulsant Activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine Derivatives

Abstract

In this study, a series of new 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives was synthesized and their anticonvulsant activity and neurotoxicity was evaluated with the maximal electroshock and rotarod tests, respectively. The most promising compounds, 3p (5-(4-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridine) and 3r (5-(4-bromophenoxy)-[1,2,4]triazolo[4,3-a]pyridine), showed a median effective dose of 13.2 and 15.8 mg/kg and had a protective index value of 4.8 and 6.9, respectively. For exploring the putative mechanism of action, compounds 3n, 3p and 3r were tested in chemically induced models.

Synthesis, crystal structure, herbicidal activities and 3D-QSAR study of some novel 1,2,4-triazolo[4,3-a ]pyridine derivatives

“…Fused heterocyclic compounds often display two heterocycle functions. It has been reported that 1,2,4‐triazolo[4,3‐ a ]pyridine possesses excellent biological activities . The incorporation of a pyridine ring into the triazole ring is considered to be a good way to produce novel active compounds.…”

Recent developments on triazole nucleus in anticonvulsant compounds: a review

“…Meanwhile, the synthesis and anticonvulsant evaluation of a series of 5-alkoxy-[1,2,4] triazolo[4,3-a]pyridines ( 86 , Figure 13 ) were carried out by Guan and coworkers. Based on the MES test and rotarod test, compounds 86a ( Figure 13 ) and 86b ( Figure 13 ) showed promising anticonvulsant activity with an ED 50 of 13.2 and 15.8 mg/kg and had a protective index value of 4.8 and 6.9, respectively 109 .…”

A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation

“…As a follow up to our previous study [ 10 ], in collaboration with Laboratory of Microbiology, Parasitology and Hygiene, University of Antwerp, we paid attention to triazolopyridine scaffold bearing sulfonamide group as chemical entity with potential antimalarial activity. Triazolopyridines represents an important class of heteroaromatic compounds with a wide range of pharmaceutical and biological activities including antibacterial, antifungal [ 11 ], anti-inflammatory [ 12 , 13 , 14 ], herbicidal [ 15 ] and pesticidal [ 16 ], anticonvulsant [ 17 ], anxiolytic [ 18 ], and antipsychotic [ 19 ]. Triazolopyridine compounds bearing sulfonamide substituent are useful for the treatment of cystic fibrosis [ 20 , 21 ].…”