38603-77-9Relevant articles and documents
Imidazole-based pinanamine derivatives: Discovery of dual inhibitors of the wild-type and drug-resistant mutant of the influenza A virus
Dong, Jianghong,Chen, Shengwei,Li, Runfeng,Cui, Wei,Jiang, Haiming,Ling, Yixia,Yang, Zifeng,Hu, Wenhui
, p. 605 - 615 (2015/12/30)
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.
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor α (TNF-α) production: Selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3- carbonitriles
Green, Neal,Hu, Yonghan,Janz, Kristin,Li, Huan-Qiu,Kaila, Neelu,Guler, Satenig,Thomason, Jennifer,Joseph-McCarthy, Diane,Tam, Steve Y.,Hotchandani, Rajeev,Wu, Junjun,Huang, Adrian,Wang, Qin,Leung, Louis,Pelker, Jefferey,Marusic, Suzana,Hsu, Sang,Telliez, Jean-Baptiste,Hall, J. Perry,Cuozzo, John W.,Lin, Lih-Ling
, p. 4728 - 4745 (2008/03/11)
Tumor progression loci-2 (Tpl2) (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family directly upstream of MEK. Recent studies using Tpl2 knockout mice have indicated an important role for Tpl2 in the lipopolysaccharide (LPS) induced production of
Imidazotriazines as Potential Antiasthma Agents
Paul, Rolf,Brockman, John A.,Hallett, W. A.,Hanifin, John W.,Tarrant, M. Ernestine,et al.
, p. 1704 - 1716 (2007/10/02)
By using inhibition of histamine release from antigen-challenged, sensitized human basophils as a means of identifying a potentialy prophylactic drug for the treatment of asthma, a series of substituted imidazotriazines were found, which wer
PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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, (2015/12/08)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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, (2015/12/08)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
-
, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
