Optimization of Imidazole 5-Lipoxygenase Inhibitors and Selection and Synthesis of a Development Candidate

概要

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Structural modification of imidazole 5-lipoxygenase (5-LO) inhibitors for optimizing inhibitory potency, pharmacokinetic behavior and toxicity (ocular) profile led to 4-{3-[4-(2-methyl-1H-imidazol-1-yl) phenylthio]} phenyl-3, 4, 5, 6-tetrahydro-2H-pyran-4-carboxamide (6) with no observable ocular toxicity. The orally active and safe imidazole 5-LO inhibitor 6 was selected as a clinical candidate and advanced to clinical studies. An improved synthesis of 6 is also discussed.
公益社団法人日本薬学会の論文
2005-08-01