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4-Amidinophenyl-benzoates

For preparation of a wide range of acyl derivatives of trypsinlike enzymes, the 4-amidinophenyl benzoates proved appropriate, and using these fools preparation of acyl enzymes is relatively easy. In the first step the enzyme is acylatcd in the presence of excessive ester concentrations. Thereafter deacylation is stopped by lowering pH and temperature. Ultimately, the acyl enzyme is isolated from the... [Pg.55]

Rgura 2 Schematic representation of acylation of serine proteases by amidinophenyl benzoates deacy Ution rate (ka) depends on benzoic add subsiitutkm (R). [Pg.55]

More recently, these esters increased in significance for the preparation of stable acyl enzymes, which regain their activity by deacylation and, accordingly, have prodrug characteristics. Therefore, we have continued our investigations into amidinophenyl benzoates in order to prepare acylated serine proteases of pharmacological interest (Table 1). [Pg.55]


See other pages where 4-Amidinophenyl-benzoates is mentioned: [Pg.54]    [Pg.62]    [Pg.54]    [Pg.62]    [Pg.66]   
See also in sourсe #XX -- [ Pg.54 , Pg.62 , Pg.66 ]




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