256461-75-3Relevant academic research and scientific papers
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors
Terasaka, Tadashi,Okumura, Hiroyuki,Tsuji, Kiyoshi,Kato, Takeshi,Nakanishi, Isao,Kinoshita, Takayoshi,Kato, Yasuko,Kuno, Masako,Seki, Nobuo,Naoe, Yoshinori,Inoue, Takeshi,Tanaka, Kohichiro,Nakamura, Katsuya
, p. 2728 - 2731 (2007/10/03)
We disclose optimization efforts based on the novel non-nucleoside adenosine deaminase (ADA) inhibitor, 4 (Ki = 680 nM). Structure-based drug design utilizing the crystal structure of the 4/ADA complex led to discovery of 5 (Ki = 11
Imidazole compounds
-
Page column 28, (2008/06/13)
Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s); R2is hydrogen or lower alkyl; R3is hydroxy or protected hydroxy; R4is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and —A— is —Q— or —O—Q—, wherein Q is single bond or lower alkylene, provided that when R2is lower alkyl, then R1is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
