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

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

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(3), pp.271-274 [Peer Reviewed Journal]

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  • Title:
    Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase
  • Author: 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
  • Description: 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 ( k inact / K i in the range 217,000–1,326,000 M −1 s −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. 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 ( k inact / K i in the range 217,000–1,326,000 M −1 s −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.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(3), pp.271-274
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/0960-894X(95)00022-L
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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