Journal of Pharmaceutical Sciences p. 977 - 980 (1988)
Update date:2022-08-04
Topics:
Martini
Marrucci
Lucacchini
Biagi
Livi
Certain 1,2,3-triazole derivatives were prepared and tested for their ability to displace [3H]diazepam from bovine brain membranes. From these compounds, the quinolyltriazole derivatives (14, 15, 16, 17) were clearly the most potent, while the naphthyl- and the naphthyridyl-triazoles were considerably less active. The p-nitrophenyl derivative (15) was the compound that bound with the highest affinity within the quinolyltriazole compounds class. The replacement of the p-nitrophenyl group with other substituents greatly decreased the binding activity. From a Lineweaver-Burk analysis of 11, it appears that the inhibition is competitive.
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