New compounds with biological activity based on hydroxy‐amino derivatives of benzoxazolyl‐2‐mercaptoformic acid, benzoxazolyl‐2‐mercaptoacetic acid, and chloracetyl‐2‐mercaptobenzoxazole have been synthesized. The chemical bonding of these compounds to poly(maleic anhydride‐alt‐vinyl acetate), through esterification, leads in obtaining conjugates of polymer biologically active compound type, tests indicating a sustained release of the active chemical, with time (between 5 and 6 h). Reaction products were characterized through elemental and spectral analysis (FTIR and 1H NMR). Toxicology and antimicrobial activity tests recommend compounds with small molecule, as well as their conjugates as therapeutical candidates (antimicrobial inhibitors) for pharmacological application.