Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.

@article{Settimo2005NovelHP,
  title={Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.},
  author={Federico Da Settimo and Giampaolo Primofiore and Concettina La Motta and Sabrina Taliani and Francesca Simorini and Anna Maria Marini and Laura Mugnaini and Antonio Lavecchia and Ettore Novellino and Daniela Tuscano and Claudia Martini},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 16},
  pages={
          5162-74
        }
}
This study reports the synthesis of a number of 1- and 2-alkyl derivatives of the 4-aminopyrazolo[3,4-d]pyrimidine (APP) nucleus and their evaluation as inhibitors of ADA from bovine spleen. The 2-substituted aminopyrazolopyrimidines proved to be potent inhibitors, most of them exhibiting K(i) values in the nanomolar/subnanomolar range. In this series the inhibitory activity is enhanced with the increase in length of the alkyl chain, reaching a maximum with the n-decyl substituent. Insertion of… CONTINUE READING

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