Title of article :
Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase
Author/Authors :
Philippe L. Durette، نويسنده , , Renee M. Chabin، نويسنده , , Daniel S. Fletcher، نويسنده , , Barbara G. Green، نويسنده , , William A. Hanlon، نويسنده , , John L. Humes، نويسنده , , Wilson B. Knight، نويسنده , , Thomas J. Lanza Jr.، نويسنده , , Richard A. Mumford، نويسنده , , Stephen Pacholok، نويسنده , , Malcolm MacCoss، نويسنده ,
Abstract :
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.
