Cyclopropenone-containing cysteine proteinase inhibitors. Synthesis and enzyme inhibitory activities
β Scribed by Ryoichi Ando; Toshiro Sakaki; Yasuhiro Morinaka; Chizuko Takahashi; Yoshikuni Tamao; Narihiko Yoshii; Sota Katayama; Ken-ichi Saito; Hidetoshi Tokuyama; Masahiko Isaka; Eiichi Nakamura
- Book ID
- 108480714
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- English
- Weight
- 205 KB
- Volume
- 7
- Category
- Article
- ISSN
- 0968-0896
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An indolizidinone motif with strategically placed substitutents was designed and synthesized as a constrained mimic of D-Phe-Pro-Arg. Low nanomolar inhibition of alpha-thrombin validates the design elements in this inhibitor which also exhibits a 20-fold selectivity for thrombin versus trypsin. An X
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