Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.

@article{Soyka1999GuanidineDA,
  title={Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.},
  author={Rainer Soyka and Brian D. Guth and H M Weisenberger and Peter Luger and Tilko H D M{\"u}ller},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 7},
  pages={1235-49}
}
A new series of omega-disubstituted alkenoic acid derivatives derived from samixogrel 5 were designed and synthesized as combined thromboxane A2 receptor antagonists/thromboxane A2 synthase inhibitors with improved solubility and reduced protein binding compared to 5. Hexenoic acid derivatives with a 3-pyridyl group and 3-(2-cyano-3-alkyl-guanidino)phenyl substituent were found to be optimal with regard to this dual mode of action. The most potent compound, E-6-(3-(2-cyano-3-tert-butyl… CONTINUE READING