In search of an effective antibacterial agent that is useful in photodynamic therapy, new derivatives of zirconium(IV) phthalocyanine (ZrPc) complexes were obtained and linked to graphite oxide flakes. In the syntheses of ZrPc derivatives, two bis-axially substituted ligands with terminal amino group and different lengths of linear carbon chain (C4 in 4-aminobutyric acid or C11 in 11-aminoundecanoic acid) were used. The optical properties (absorption and photoluminescence spectra) of ZrPcs and the composites were examined. Broadband red–near-infrared lamp was tested as an external stimulus to activate ZrPcs and the composites. Optical techniques were used to show generation of singlet oxygen during irradiation. Considering the application of graphite oxide-based materials as bacteriostatic photosensitive additives for endodontic treatment of periapical tissue inflammation, the antibacterial activity was determined on one Escherichia coli strain isolated directly from an infected root canal of a human tooth and one strain with silver and antibiotic resistance. Looking at the obtained results, modified levels of activity toward different bacterial strains are discussed.