Based on a pharmacophore model of the benzodiazepine-binding site of GABA(A) receptors, a series of 2-aryl-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-diones (structure type I) were designed, synthesized, and identified as high-affinity ligands of the binding site. For several compounds, K(i) values of around 0.20nM were determined. They show a structural resemblance with the previously described 2-phenyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones (II) and 2-phenyl-[1,2,4]triazolo[1,5-a]quinoxalin-4(5H)-one (III). The 9-bromo substituted compounds 8a-d were prepared in an 8-step synthesis in an overall yield of approximately 40%, and a library of 9-substituted analogues was prepared by cross-coupling reactions. Compound 8e, 21, 22, and 24 w...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones (PQ, 106 compound...
The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzo...
This paper reports the synthesis and evaluation of the biological affinity towards benzodiazepine an...
Ligands for the benzodiazepine-binding site of the GABAA receptor can belong to structurally diverse...
The 3-ethoxycarbonyl-4-quinolone compound I has previously been identified via a database search as ...
This paper reports the synthesis and binding assays toward benzodiazepine and adenosine A(1) and A(2...
Based on a pharmacophore model of the benzodiazepine binding site of the GABA(A) receptors, develope...
The finding that alkyl 1,4-dihydro-4-oxoquinoline-3-carboxylate and N-alkyl-1,4-dihydro-4-oxoquinoli...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
The synthesis, the benzodiazepine binding activity and the ''in vitro'' biological effect of some 1,...
On pursuing research about 1,2,3-triazolo[1,5-a]quinoxalines. in this paper we report synthesis and ...
A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the cen...
Structure activity relationship studies of synthetic flavone derivatives have been utilized to refin...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones (PQ, 106 compound...
The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzo...
This paper reports the synthesis and evaluation of the biological affinity towards benzodiazepine an...
Ligands for the benzodiazepine-binding site of the GABAA receptor can belong to structurally diverse...
The 3-ethoxycarbonyl-4-quinolone compound I has previously been identified via a database search as ...
This paper reports the synthesis and binding assays toward benzodiazepine and adenosine A(1) and A(2...
Based on a pharmacophore model of the benzodiazepine binding site of the GABA(A) receptors, develope...
The finding that alkyl 1,4-dihydro-4-oxoquinoline-3-carboxylate and N-alkyl-1,4-dihydro-4-oxoquinoli...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying approp...
The synthesis, the benzodiazepine binding activity and the ''in vitro'' biological effect of some 1,...
On pursuing research about 1,2,3-triazolo[1,5-a]quinoxalines. in this paper we report synthesis and ...
A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the cen...
Structure activity relationship studies of synthetic flavone derivatives have been utilized to refin...
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones (PQ, 106 compound...
The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzo...
This paper reports the synthesis and evaluation of the biological affinity towards benzodiazepine an...