Abstract
SummaryNovelty: Novel benzoic acid phenylesters which have a substituted amino group at position 4, are disclosed. The compounds are said to be inhibitors of human leukocyte elastase. Elastase inhibiting compositions which contain the compounds are also disclosed.Biology: In vitro human leukocyte elastase inhibition is demonstrated for a number of representative compounds (IC50 = 0.57 μM to 1.3 nM).Chemistry: The compounds can be produced by converting a 4-aminobenzoic acid phenylester to a corresponding amide, imide, urea or urethane compound. The preparation of 3,5-dichlorophenyl 4-(isobutanoylamino)benzoate; 3,5-dichlorophenyl 4-(3-butylureido)-benzoate and 3-formyl-6-nitrophenyl 4-(pivaloylamino)benzoate are exemplified. A total of ninety-four compounds are listed together with characterization data.Structure:
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