Synthesis and structure-activity study of protease inhibitors. III. Amidinophenols and their benzoyl esters.

@article{Yaegashi1984SynthesisAS,
  title={Synthesis and structure-activity study of protease inhibitors. III. Amidinophenols and their benzoyl esters.},
  author={Takashi Yaegashi and Shigeki Nunomura and Toshiyuki Okutome and Toyoo Nakayama and Masateru Kurumi and Youji Sakurai and Takuo Aoyama and Setsuro Ebiya-Cho Fujii},
  journal={Chemical \& pharmaceutical bulletin},
  year={1984},
  volume={32 11},
  pages={
          4466-77
        }
}
Various amidinophenol derivatives (27-47) and their benzoates (4-26) were synthesized and evaluated for inhibitory activities against trypsin, plasmin, kallikrein, thrombin, Clr and Cls as well as in vitro complement-mediated hemolysis. 4-(β-Amidinoethenyl) phenyl 4-guanidinobenzoate (15) and 4-amidino-2-benzoylphenyl 4-guanidinobenzoate (26) were found to have potent inhibitory activities with IC50s of 9×10-8M (trypsin) and 2×10-7M (Cls) for the former and 3×10-8M (trypsin) and 2×10-7M (Cls… 
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