- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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- Imidazole-based pinanamine derivatives: Discovery of dual inhibitors of the wild-type and drug-resistant mutant of the influenza A virus
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We previously reported potent hit compound 4 inhibiting the wild-type influenza A virus A/HK/68 (H3N2) and A/M2-S31N mutant viruses A/WS/33 (H1N1), with its latter activity quite weak. To further increase its potency, a structure-activity relationship study of a series of imidazole-linked pinanamine derivatives was conducted by modifying the imidazole ring of this compound. Several compounds of this series inhibited the amantadine-sensitive virus at low micromolar concentrations. Among them, 33 was the most potent compound, which was identified as being active on an amantadine-sensitive virus through blocking of the viral M2 ion channel. Furthermore, 33 markedly inhibited the amantadine-resistant virus (IC50 = 3.4 μM) and its activity increased by almost 24-fold compared to initial compound, with its action mechanism being not M2 channel mediated.
- Dong, Jianghong,Chen, Shengwei,Li, Runfeng,Cui, Wei,Jiang, Haiming,Ling, Yixia,Yang, Zifeng,Hu, Wenhui
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p. 605 - 615
(2015/12/30)
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- Analgesic, antipyretic or anti-inflammatory imidazole compounds
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New imidazole compounds of the formula STR1 their salts and analgesic, antipyretic and antiinflammatory pharmaceutical composition containing them. New intermediates useful in the preparation of said imidazole compounds. Process for preparing the new imid
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- Synthesis of 4(5)-Hydroxymethylimidazoles by Hydroxymethylation and Decarboxylation of Imidazole-4(5)-carboxylic Acids
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4(5)-Hydroxymethylimidazoles were prepared by hydroxymethylation and decarboxylation of imidazole-4(5)-carboxylic acid esters.The reaction was simply carried out with aqueous formaldehyde solution in the presence of base.
- Kim, Choong S.,Lee, Kee J.,Kim, Hong S.,Chae, Yung B.
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p. 1417 - 1418
(2007/10/02)
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