Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase

…, IA Schepetkin, A Cilibrizzi, A Graziano…

文献索引：Crocetti, Letizia; Schepetkin, Igor A.; Cilibrizzi, Agostino; Graziano, Alessia; Vergelli, Claudia; Giomi, Donatella; Khlebnikov, Andrei I.; Quinn, Mark T.; Giovannoni, Maria Paola Journal of Medicinal Chemistry, 2013 , vol. 56, # 15 p. 6259 - 6272

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被引用次数: 16

摘要

Human neutrophil elastase (HNE) is an important therapeutic target for treatment of pulmonary diseases. Previously, we identified novel N-benzoylindazole derivatives as potent, competitive, and pseudoirreversible HNE inhibitors. Here, we report further development of these inhibitors with improved potency, protease selectivity, and stability compared to our previous leads. Introduction of a variety of substituents at position 5 of the ...