Abstract
Whether or not functionalized PEGs may be useful in the case of low molecular weight drugs has not yet been examined so far. For that purpose captopril, a thiol containing drug, was converted into a prodrug, captopril-S-S-PEG, which does not inhibit ACE activity. The inhibitory action of captopril-SH can be regenerated by chemical reduction (gluthatione, DTT or NaBH4) of that prodrug. Yet, as those chemical reagents themselves partially inhibit ACE activity, the inhibitory effect of the freed captopril-SH alone was shown to be fully recovered after coulometric reduction.
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