On January 31, 2021, Navidpour, Latifeh; Shabani, Shabnam; Heidari, Alireza; Bashiri, Manouchehr; Ebrahim-Habibi, Azadeh; Shahhosseini, Soraya; Shafaroodi, Hamed; Abbas Tabatabai, Sayyed; Toolabi, Mahsa published an article.Recommanded Product: 99-60-5 The title of the article was 5-[Aryloxypyridyl (or nitrophenyl)]-4H-1,2,4-triazoles as novel flexible benzodiazepine analogues: Synthesis, receptor binding affinity and lipophilicity-dependent anti-seizure onset of action. And the article contained the following:
A new series of 5-(2-aryloxy-4-nitrophenyl)-4H-1,2,4-triazoles and 5-(2-aryloxy-3-pyridyl)-4H-1,2,4-triazoles, possessing C-3 thio or alkylthio substituents, was synthesized and evaluated for their benzodiazepine receptor affinity and anti-seizure activity. These analogs revealed similar to significantly superior affinity to GABAA/benzodiazepine receptor complex (IC50 values of 0.04-4.1 nM), relative to diazepam as the reference drug (IC50 value of 2.4 nM). To determine the onset of anti-seizure activity, the time-dependent effectiveness of i.p. administration of compounds on pentylenetetrazole induced seizure threshold was studied and a very good relationship was observed between the lipophilicity (cLogP) and onset of action of studied analogs (r2 = 0.964). The min. ED of the compounds, determined at the time the analogs showed their highest activity, was demonstrated to be 0.025-0.1 mg/kg, relative to diazepam (0.025 mg/kg). The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Recommanded Product: 99-60-5
The Article related to triazol flexible benzodiazepine derivative preparation lipophilicity antiseizure activity, 1,2,4-triazole, flexible benzodiazepines, gabaa/benzodiazepine receptor complex, onset of action, ptz induced seizure threshold and other aspects.Recommanded Product: 99-60-5
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