DOI: 10.1039/d6md00430j ISSN: 2632-8682

Development of atropisomeric 5 N -sulfonyl-1,5-benzodiazepin-2-ones with high inhibitory activity against neutrophil elastase

Hidetsugu Tabata, Yoshiki Miyata, Yoshio Kusakabe, Hideyo Takahashi, Hideaki Natsugari, Tetsuta Oshitari

Novel N -sulfonyl-1,5-benzodiazepin-2-one derivatives (2d) were designed based on Sivelestat (1). The a R , a R atropisomer exhibited approximately 10-fold higher inhibitory activity against neutrophil elastase than Sivelestat.

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