Author/Authors :
Masahiro Eda، نويسنده , , Atsuyuki Ashimori، نويسنده , , Fumihiko Akahoshi، نويسنده , , Takuya Yoshimura، نويسنده , , Yoshihisa Inoue، نويسنده , , Chikara Fukaya، نويسنده , , Masahide Nakajima، نويسنده , , Hajime Fukuyama، نويسنده , , Teruaki Imada، نويسنده , , Norifumi Nakamura، نويسنده ,
Abstract :
Appropriate structural modification of the difluoromethylene ketone derivatives at both P3 and P′ positions led us to the discovery of peptidyl human heart chymase inhibitor 12h which shows potent activity with Ki = 6 nM and high selectivity against closely related serine protease bovine α-chymotrypsin (chymotrypsin Ki = >100 μM). Using the compound 12b, a docking study with human heart chymase was carried out to presume probable interactions.
