Synthesis and evaluation of a β-lactam-containing dipeptide analog as a protease inhibitor

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 8, 1996, Pages 983-986

  Wu, Zhijun ^a   Georg, Gunda I ^a   Cathers, Brian E ^a   Schloss, John V ^a  

^a UNIVERSITY OF KANSAS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA LACTAM DERIVATIVE; CATHEPSIN G; CHYMOTRYPSIN A; ELASTASE; ENZYME INHIBITOR; PROTEINASE INHIBITOR; PROTEINASE K; SERINE CARBOXYPEPTIDASE;

ARTICLE; DRUG SYNTHESIS; ENZYME INHIBITION;

EID: 0029874671     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00153-9     Document Type: Article

References (19)

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10. All compounds displayed spectroscopic and analytical data in accordance with their structures.
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15. Assay conditions: buffer = 0.1 M tris(hydroxymethyl)-aminomethane (Tris) pH 7.5; substrate = 0.1 M succinyl-alanyl-alanyl-prolyl-phenylalanyl-para-nitroanilide (Suc-AAPF-pNA).
16. Assay conditions: buffer = 0.1 M tris(hydroxymethyl)-aminomethane (Tris) pH 8.0; substrate = 0.08 M succinyl-alanyl-alanyl-alanyl-para-nitroanilide (Suc-AAA-pNA).
17. 2; substrate = 0.1 M succinyl-alanyl-alanyl-prolyl-phenylalanyl-para-nitroanilide (Suc-AAPF-pNA).
18. Assay conditions: buffer = 0.05 M 2-(N-morpholino)ethanesulfonic acid (MES) pH 6.2; substrate = 0.5 M N-benzoyl-tyrosyl-para-nitroanilide (BTNA).
19. Concentration of 1 that produces one-half maximal enzyme activity.