Author/Authors :
Hidekazu Masaki، نويسنده , , Yusuke Mizuno، نويسنده , , Akira Tatui، نويسنده , , Akira Murakami، نويسنده , , Yuuki Koide، نويسنده , , Shoji Satoh، نويسنده , , Atsuo Takahashi، نويسنده ,
Abstract :
We have identified a new class of chymase inhibitor through a substituent analysis of MWP00965, which we previously discovered by in silico screening. TY-51076 (7) showed high potency (IC50=56 nM) and excellent selectivity for chymase compared to chymotrypsin and cathepsin G (>400-fold). The synthesis and structure–activity relationship of this class are described.