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

…, IA Schepetkin, A Cilibrizzi, A Graziano…

Index: 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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Citation Number: 16

Abstract

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 ...