- Synthesis and potent antifungal activity against Candida species of some novel 1H-benzimidazoles
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(Chemical Equation Presented) A series of 47 novel N1-alkylated- 2-aryl-5(6)-substituted-1H-benzimidazoles and their three novel indole analogues were synthesized and evaluated for in vitro antifungal activities against Candida species by the tube dilution method. The results showed that compounds 79 and 80, having pyridine at the position C-2, of benzimidazoles exhibited the greatest activity with MIC values of 6.25-3.12 μg/mL. Indole analogues 108-110 have no inhibitory activity.
- Goeker, Hakan,Alp, Mehmet,Ates-Alagoez, Zeynep,Yildiz, Sulhiye
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experimental part
p. 936 - 948
(2009/12/05)
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- Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
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Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
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- EP4 RECEPTOR INHIBITORS TO TREAT RHEUMATOID ARTHRITIS
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The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin EP4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.
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- Cardiotonic Agents. Synthesis and Cardiovascular Properties of Novel 2-Arylbenzimidazoles and Azabenzimidazoles
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Novel 2-arylbenzimidazoles and azabenzimidazoles were synthesized, and their inotropic action was evaluated.Changes in left ventricular pressure, dP/dt max, were measured as an index of cardiac contractility.The structural features that impart optimal inotropic activity are presented.The most potent compounds were evaluated orally in conscious dogs with implanted Konigsberg pressure transducers.To investigate the mechanism of action, the most potent compounds were tested for their calcium-sensitizing properties and their potential for the inhibition of phosphodiesterase.Two compounds, 1 and 41, showed interesting in vitro and oral activity without side effects.They have a more potent calcium-sensitizing effect than MCI-154 and are under further investigation.
- Guengoer, Timur,Fouquet, Andre,Teulon, Jean-Marie,Provost, Daniel,Cazes, Michele,et al.
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p. 4455 - 4463
(2007/10/02)
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- N-(Aminophenyl)oxamic Acids and Esters as Potent, Orally Active Antiallergy Agents
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A series of N-(2-cyano-substituted-phenyl)oxamates was prepared by acylation of the appropriate anthranilonitrile with ethyloxalyl chloride.Hydrolysis with sodium hydroxide gave the corresponding oxamic acid sodium salts.These compounds were extremely potent when tested in the rat passive cutaneous anaphylaxis (PCA assay either by the ip or the po route of administration).One of the sodium salts, oxoacetic acid sodium salt (11a, Wy-41 195), has ED50 value of 0.07 mg/kg po and has been selected for further evaluation.
- Klaubert, Dieter H.,Sellstedt, John H.,Guinosso, Charles J.,Capetola, Robert J.,Bell, Stanley C.
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p. 742 - 748
(2007/10/02)
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