Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
نویسندگان
چکیده
Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamster liver microsomes, the introduction of aqueous solubility through the piperidine salt 9, the in vivo oral activity of 9 and its bioavailability, and the introduction of 9 as an intracellular neutrophil elastase inhibitor.
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 11 2 شماره
صفحات -
تاریخ انتشار 2001