Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase

Autor: Durette, Philippe L., Chabin, Renee M., Fletcher, Daniel S., Green, Barbara G., Hanlon, William A., Humes, John L., Knight, Wilson B., Lanza, Thomas J., Mumford, Richard A., Pacholok, Stephen, MacCoss, Malcolm
Zdroj: Bioorganic & Medicinal Chemistry Letters; 1995, Vol. 5 Issue: 3 p271-274, 4p
Abstrakt: Analogs of the monocyclic β-lactam human leukocyte elastase (HLE) inhibitor L-680,833 in which the carboxyl group is replaced by phosphorous acid moieties were synthesized and found to be potent inhibitors of the enzyme (kinact/Ki in the range 217,000–1,326,000 M−1s−1). Cellular activity was demonstrated by inhibition of the generation of the N-terminal cleavage product Aα-(1–21) from the Aα chain of fibrinogen.
Databáze: Supplemental Index