Inhibition of serine proteinases by benzamidine derivatives. 1977

P Walsmann

Derivatives of benzamidine inhibit competitively the activity of the serine proteinases trypsin, plasmin, thrombin, and of the clotting factor Xa. The inhibitor activities (Ki-values) of various benzamidine derivatives against the several enzymes were compared. Besides parallels, deviations in the corresponding structure-activity relationships were found. From these results it is concluded that the similar enzymes exhibit certain differences in the structure of the primary and secondary binding sites.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D011480 Protease Inhibitors Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES). Antiprotease,Endopeptidase Inhibitor,Endopeptidase Inhibitors,Peptidase Inhibitor,Peptidase Inhibitors,Peptide Hydrolase Inhibitor,Peptide Hydrolase Inhibitors,Peptide Peptidohydrolase Inhibitor,Peptide Peptidohydrolase Inhibitors,Protease Antagonist,Protease Antagonists,Antiproteases,Protease Inhibitor,Antagonist, Protease,Antagonists, Protease,Hydrolase Inhibitor, Peptide,Hydrolase Inhibitors, Peptide,Inhibitor, Endopeptidase,Inhibitor, Peptidase,Inhibitor, Peptide Hydrolase,Inhibitor, Peptide Peptidohydrolase,Inhibitor, Protease,Inhibitors, Endopeptidase,Inhibitors, Peptidase,Inhibitors, Peptide Hydrolase,Inhibitors, Peptide Peptidohydrolase,Inhibitors, Protease,Peptidohydrolase Inhibitor, Peptide,Peptidohydrolase Inhibitors, Peptide
D000578 Amidines Derivatives of oxoacids RnE(
D001550 Benzamidines Amidines substituted with a benzene group. Benzamidine and its derivatives are known as peptidase inhibitors.
D012694 Serine A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids. L-Serine,L Serine
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships

Related Publications

P Walsmann
January 1980, Hoppe-Seyler's Zeitschrift fur physiologische Chemie,
P Walsmann
January 1986, Toxicon : official journal of the International Society on Toxinology,
P Walsmann
March 1993, Thrombosis research,
P Walsmann
July 1990, Biological chemistry Hoppe-Seyler,
P Walsmann
April 1997, The Journal of biological chemistry,
P Walsmann
January 1971, Farmakologiia i toksikologiia,
P Walsmann
January 1992, Agents and actions. Supplements,
P Walsmann
October 1992, Biological chemistry Hoppe-Seyler,
Copied contents to your clipboard!