Looking at the pharmacological importance of 8‐hydroxyquinolines and sulfonamides, in the present study, a novel bi‐dentate ligand 4‐amino‐N′‐[(8‐hydroxyquinoline‐5‐yl)methyl] benzenesulfonohydrazide (AHQMBSH) having above both moieties within a single molecular framework was synthesized by the reaction of N‐acetamidobenzene sulfonohydrazide with 5‐chloromethyl‐8‐hydroxyquinoline hydrochloride. Its metal(II) oxinates were also prepared with Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II) salts. All the above compounds were investigated by physicochemical analyses, thermogravimetric analysis and spectroscopic techniques. Antimicrobial activities for the above prepared compounds were carried out using the agar‐plate method against various strains of bacteria (Staphylococcus aureus, Bacillus subtillis, Pseudomonas aerugionsa, Escherichia coli) and fungi (Aspergillus niger and Aspergillus flavous). The results show a significant increase in antimicrobial and antifungal activities of AHQMBSH compared with the parent 8‐hydroxyquinoline and sulfonamides. Copyright © 2010 John Wiley & Sons, Ltd.