New anti-inflammatory N-pyridinyl (alkyl) phthalimides acting as tumour necrosis factor-α production inhibitors

…, G Wielgosz, G Le Baut, C Bobin-Dubigeon…

文献索引：Collin, Xavier; Robert, Jean-Michel; Wielgosz, Gaetane; Le Baut, Guillaume; Bobin-Dubigeon, Christine; Grimaud, Nicole; Petit, Jean-Yves European Journal of Medicinal Chemistry, 2001 , vol. 36, # 7-8 p. 639 - 649

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被引用次数: 79

摘要

This paper describes the synthesis of N-pyridinyl (alkyl) phthalimides related to N-phenyl-4, 5, 6, 7-tetrafluorophthalimides known to be inhibitors of tumour necrosis factor-α (TNFα) production. Pharmacomodulation at the phthalimidic nitrogen led to the selection of two pharmacophoric fragments (2, 4-lutidinyl and β-picolyl), allowing significant inhibition of TNFα production (compounds 12 and 17). Variation of the substituents linked to the ...