An insight into the pharmacophores of phosphodiesterase-5 inhibitors from synthetic and crystal structural studies.

@article{Chen2008AnII,
  title={An insight into the pharmacophores of phosphodiesterase-5 inhibitors from synthetic and crystal structural studies.},
  author={Gong Chen and Huanchen Wang and Howard Robinson and Jiwen Cai and Yiqian Wan and Hengming Ke},
  journal={Biochemical pharmacology},
  year={2008},
  volume={75 9},
  pages={1717-28}
}
Selective inhibitors of cyclic nucleotide phosphodiesterase-5 (PDE5) have been used as drugs for treatment of male erectile dysfunction and pulmonary hypertension. An insight into the pharmacophores of PDE5 inhibitors is essential for development of second generation of PDE5 inhibitors, but has not been completely illustrated. Here we report the synthesis of a new class of the sildenafil derivatives and a crystal structure of the PDE5 catalytic domain in complex with 5-(2-ethoxy-5-(sulfamoyl)-3… CONTINUE READING

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