Pyrimidines

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Geoffrey Heinzl - One of the best experts on this subject based on the ideXlab platform.

Xinhua He - One of the best experts on this subject based on the ideXlab platform.

Hongbin Tu - One of the best experts on this subject based on the ideXlab platform.

Shaymaa E Kassab - One of the best experts on this subject based on the ideXlab platform.

Javier Forn - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and sar of a new series of cox 2 selective inhibitors pyrazolo 1 5 a Pyrimidines
    Journal of Medicinal Chemistry, 2001
    Co-Authors: Carmen Almansa, Alberto Fernandez De Arriba, Fernando L Cavalcanti, Luis A Gomez, Agusti Miralles, Manuel Merlos, Julian Garciarafanell, Javier Forn
    Abstract:

    The synthesis and pharmacological activity of a series of bicyclic pyrazolo[1,5-a]Pyrimidines as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema and air-pouch model). Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6,7-dimethyl-2-(4-methylsulfonylphenyl)pyrazolo[1,5-a]pyrimidine (10f) as one of the most potent and selective COX-2 inhibitor in this series.