4 research outputs found
Solid Phase Synthesis of 1,5-Diarylpyrazole-4-carboxamides: Discovery of Antagonists of the CB-1 Receptor
We have developed a solid phase synthesis route to 1,5-substituted
pyrazole-4-carboxamides with three diversity points aimed at the discovery
of new compounds as potential G-Protein coupled receptor (GPCR) ligands.
The new chemistry involves acylation of a resin bound secondary amine
with a β-ketoester via transamidation, conversion of the resulting
β-ketoamide to the corresponding vinylogous amide, pyrazole
formation upon reaction with a aryl hydrzine, and cleavage of the
product from the resin. Using the reported methodology, we describe
the syntheses of multiple arrays of pyrazoles that were used collectively
to construct a library of more than 1000 analogues. Several members
of this library displayed submicromolar antagonist activities at the
cannabinoid subtype 1 (CB-1) receptor
Solid Phase Synthesis of 1,5-Diarylpyrazole-4-carboxamides: Discovery of Antagonists of the CB-1 Receptor
We have developed a solid phase synthesis route to 1,5-substituted
pyrazole-4-carboxamides with three diversity points aimed at the discovery
of new compounds as potential G-Protein coupled receptor (GPCR) ligands.
The new chemistry involves acylation of a resin bound secondary amine
with a β-ketoester via transamidation, conversion of the resulting
β-ketoamide to the corresponding vinylogous amide, pyrazole
formation upon reaction with a aryl hydrzine, and cleavage of the
product from the resin. Using the reported methodology, we describe
the syntheses of multiple arrays of pyrazoles that were used collectively
to construct a library of more than 1000 analogues. Several members
of this library displayed submicromolar antagonist activities at the
cannabinoid subtype 1 (CB-1) receptor
Solid Phase Synthesis of 1,5-Diarylpyrazole-4-carboxamides: Discovery of Antagonists of the CB-1 Receptor
We have developed a solid phase synthesis route to 1,5-substituted
pyrazole-4-carboxamides with three diversity points aimed at the discovery
of new compounds as potential G-Protein coupled receptor (GPCR) ligands.
The new chemistry involves acylation of a resin bound secondary amine
with a β-ketoester via transamidation, conversion of the resulting
β-ketoamide to the corresponding vinylogous amide, pyrazole
formation upon reaction with a aryl hydrzine, and cleavage of the
product from the resin. Using the reported methodology, we describe
the syntheses of multiple arrays of pyrazoles that were used collectively
to construct a library of more than 1000 analogues. Several members
of this library displayed submicromolar antagonist activities at the
cannabinoid subtype 1 (CB-1) receptor
Solid Phase Synthesis of 1,5-Diarylpyrazole-4-carboxamides: Discovery of Antagonists of the CB-1 Receptor
We have developed a solid phase synthesis route to 1,5-substituted
pyrazole-4-carboxamides with three diversity points aimed at the discovery
of new compounds as potential G-Protein coupled receptor (GPCR) ligands.
The new chemistry involves acylation of a resin bound secondary amine
with a β-ketoester via transamidation, conversion of the resulting
β-ketoamide to the corresponding vinylogous amide, pyrazole
formation upon reaction with a aryl hydrzine, and cleavage of the
product from the resin. Using the reported methodology, we describe
the syntheses of multiple arrays of pyrazoles that were used collectively
to construct a library of more than 1000 analogues. Several members
of this library displayed submicromolar antagonist activities at the
cannabinoid subtype 1 (CB-1) receptor