- Superelectrophiles in Synthesis: Preparation of Aromatic Imides
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Aromatic carboxylic acids are found to undergo reactions with isocyanates, wherein triflic acid promotes the formation of aromatic imide products in fair to good yields. It is proposed that the carboxylic acid group directs the isocyanate electrophile to
- Kennedy, Sean H.,Schaeff, Mark N.,Klumpp, Douglas A.
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p. 14133 - 14140
(2019/10/16)
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- Phenylhomophthalimide-type NOS inhibitors derived from thalidomide
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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.
- Noguchi, Tomomi,Sano, Hiroko,Shimazawa, Rumiko,Tanatani, Aya,Miyachi, Hiroyuki,Hashimoto, Yuichi
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p. 4141 - 4145
(2007/10/03)
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- Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study
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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.
- Komoda, Masato,Kakuta, Hiroki,Takahashi, Hiroyasu,Fujimoto, Yasuyuki,Kadoya, Shizuo,Kato, Fuminori,Hashimoto, Yuichi
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p. 121 - 131
(2007/10/03)
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- 1,3(2H,4H)-Dioxoisoquinoline-4-carboxamides used as anti-inflammatory agents
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1,3(2H,4H)-Dioxoisoquinoline-4-carboxamides, nuclear unsubstituted and substituted, are prepared by reacting the appropriate homophthalimide with potassium cyanate. Secondary carboxamides are prepared by reacting homophthalimide with appropriate isocyanates, and tertiary carboxamides are prepared by aminolysis of 4-carbalkoxy compounds, which are in turn prepared by alcoholysis of the corresponding 4-carboxanilides. Corresponding 5,6,7,8-tetrahydro compounds are similarly prepared. The various 2-substituted homophthalimides are prepared by reacting homophthalic acid with appropriate amine. The 4-carboxamides are anti-inflammatory agents.
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