- Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region
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A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34 nM to >20 μM and were dependant upon both the nature of the aryl group and the hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions.
- Levy, Daniel E.,Wang, Dan-Xiong,Lu, Qing,Chen, Zheng,Perumattam, John,Xu, Yong-jin,Liclican, Albert,Higaki, Jeffrey,Dong, Hanmin,Laney, Maureen,Mavunkel, Babu,Dugar, Sundeep
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p. 2390 - 2394
(2008/09/21)
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- Structural Factors Affecting the Basicity of ω-Pyridylalkanols, ω-Pyridylalkanamides and ω-Pyridylalkylamines
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The present paper describes the preparation by conventional methods (when not available commercially) and the pKa-determination of the α-, β- and γ-isomers of pyridylethanamide, 3-pyridylpropanamide, 4-pyridylbutanamide, 5-pyridylpentanamide, pyridylmethanol, 2-pyridylethanol, 3-pyridylpropanol, 4-pyridylbutanol, 5-pyridylpentanol, pyridylmethylamine, 2-pyridylethylamine, 3-pyridylpropylamine, 4-pyridylbutylamine, and 5-pyridylpentylamine.While a field effect accounts for many variations in pKa as a function of chain length, marked inductive effects are operative in some methyl and ethyl homologs.The pKa-decreasing influence of an intramolecular H-bond is also apparent in some lower homologs belonging to the α-series.
- Mayer, Joachim M.,Testa, Bernard
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p. 1868 - 1884
(2007/10/02)
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- 11a-Methano-TXA compounds
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The present invention provides novel 11a-methano-TXA compounds and intermediates and processs for their preparation. Further provided are methods for using these novel TXA analogs as inhibitors of thromboxane synthetase, rendering these analogs useful for a variety of pharmacological purposes. These pharmacological uses include anti-inflammatory, anti-thromobitc, and anti-asthma indications.
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