1-(Fluorobenzyl)-4-amino-1H-1,2,3-triazolo[4,5-c]pyridines: Synthesis and Anticonvulsant Activity

Abstract

A series of (fluorobenzyl)triazolo[4,5-c]pyridines was synthesized and tested for activity against maximal electroshock-induced seizures in rodents. The most promising compound, 14 (BW 534U87), which is a carbon-nitrogen isoster of a purine anticonvulsant, has a profile in rodents that suggests 14 will be free of emesis and useful in the treatment of seizure disorders for which phenytoin is presently indicated.

Catalytic behavior of surfactant-containing-MCM-41 mesoporous materials for cycloaddition of 4-nitrophenyl azide

“…In addition, compounds containing 1,2,3-triazoles have shown a broad spectrum of biological activities such as antibacterial against Gram positive bacteria [37], herbicidal and fungicidal [38], antiallergic [39], anticonvulsant [40], ␤-lactamase inhibitive [41] and anti-HIV [42]. Several synthetic methods for preparing triazole derivatives have been developed.…”

Synthesis and evaluation of 1-alkyl-4-phenyl-[1,2,3]-triazole derivatives as antimycobacterial agent

“…In particular, when the reaction occurs between alkyl or aryl azides and terminal acetylenes, [1,2,3]-triazoles are obtained. [9][10][11][12][13][14][15][16][17][18][19][20][21] If the cycloaddition is thermally conduced, a 1:1 mixture of the 1,4 and 1,5-regioisomers of triazole is usually obtained. Various attempts to control the regioselectivity without much success were reported until the discovery of the copper(I)-catalyzed reaction in 2002, which exclusively yields the 1,4-disubstituted-[1,2,3]-triazole.…”

Condensed 1,2,3-triazoles (review)

“…A convenient method for the production of triazolo [4,5-d]pyrimidines 1 is the diazotization of the corresponding 4,5-diaminopyrimidines 2 [5]. The reaction takes place through an intermediate o-aminodiazonium salt with the formation of triazolo [4,5-d]pyrimidines having various substituents at positions 5 and 7 [11][12][13]. 1-Alkyl-and 1-aryltriazolopyrimidines 3 [14] and 4 [15] were obtained similarly by the diazotization of 6-amino-substituted pyrimidines.…”