Author/Authors :
Tadashi Terasaka، نويسنده , , Isao Nakanishi، نويسنده , , Katsuya Nakamura، نويسنده , , Yoshiteru Eikyu، نويسنده , , Takayoshi Kinoshita، نويسنده , , Nobuya Nishio، نويسنده , , Akihiro Sato، نويسنده , , Masako Kuno، نويسنده , , Nobuo Seki، نويسنده , , Kazuo Sakane، نويسنده ,
Abstract :
We searched for non-nucleoside inhibitors of adenosine deaminase by rational structure-based de novo design and succeeded in the discovery of 1-(1-hydroxy-4-phenyl-2-butyl)imidazole-4-carboxamide (FR221647: Ki=5.9 μM to human ADA) as a novel inhibitor with moderate activity and good pharmacokinetics compared with the known inhibitors pentostatin and EHNA.
