20863-87-0Relevant academic research and scientific papers
Thalidomide as a nitric oxide synthase inhibitor and its structural development
Shimazawa, Rumiko,Sano, Hiroko,Tanatani, Aya,Miyachi, Hiroyuki,Hashimoto, Yuichi
, p. 498 - 499 (2004)
Thalidomide has been found to exhibit weak nitric oxide synthase (NOS)-inhibitory activity. Structural development studies of thalidomide showed that some N-2,6-dimethylphenylhomophthalimide analogs possess NOS-inhibiting activity.
Phenylhomophthalimide-type NOS inhibitors derived from thalidomide
Noguchi, Tomomi,Sano, Hiroko,Shimazawa, Rumiko,Tanatani, Aya,Miyachi, Hiroyuki,Hashimoto, Yuichi
, p. 4141 - 4145 (2007/10/03)
Thalidomide shows moderate inhibitory activity toward neuronal nitric oxide synthase (nNOS) and inducible NOS (iNOS), but not toward endothelial NOS (eNOS). Structural development studies of thalidomide yielded novel phenylhomophthalimide-type NOS inhibitors with enhanced activity and different subtype selectivity.
Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study
Komoda, Masato,Kakuta, Hiroki,Takahashi, Hiroyasu,Fujimoto, Yasuyuki,Kadoya, Shizuo,Kato, Fuminori,Hashimoto, Yuichi
, p. 121 - 131 (2007/10/03)
2-(2,6-Diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (2: PIQ-22) was found to be a potent and specific inhibitor of puromycin-sensitive aminopeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibited by PIQ-22 in a non-competitive manner. Structure-activity relationship studies indicated that tautomerism of the imidobenzoylketone group in the cyclic imide moiety of the PIQ-22 skeleton is important for the inhibitory activity.
