This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula: ##STR00001## wherein: A is C or N; B is O, S, N, or CH.dbd.CH; ##STR00002## X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole; Y is H, alkyl, or halo; Z is O, S, or N; R is H, nitro, alkyl, alkoxy, halo, or CF.sub.3; R.sup.1 is alkyl, aryl, aralkyl, halo, Het-alkyl, or optionally substituted aryl; Het is ##STR00003## G is O, S, or N; R.sup.2 is H, halo, alkyl, or --OR.sup.5; R.sup.3 and R.sup.4 are H, halo, alkyl, aryl, nitro, amino, alkylsulfoamide, arylsulfoamide, cycloalkyl, heterocycle, or optionally substituted aryl; R.sup.5 is H, alkyl, --CH(R.sup.7)R.sup.8, --C(CH.sub.2).sub.nCO.sub.2R.sup.9, --C(CH.sub.3).sub.2CO.sub.2R.sup.9, CH(R.sup.7)(CH.sub.2).sub.nCO.sub.2R.sup.9, or --CH(R.sup.7)C.sub.6H.sub.4CO.sub.2R.sup.9; R.sup.6 is alkylene; R.sup.7 is H, alkyl, aryl, aralkyl, cycloalkyl, phthalic acid, or Q-alkyl; Q is ##STR00004## R.sup.8 is --CO.sub.2R.sup.11, --CONHR.sup.11, tetrazole, or --PO.sub.3R.sup.11; R.sup.9 is H, alkyl, aryl, or aralkyl; W is O, N, or S; R.sup.11 is H, alkyl, aryl, or aralkyl; n=1-6; or a pharmaceutically acceptable salt or ester form thereof.