In this study, glycerol, glycosyl, and tetraethyleneglycol monomethyl ether group substituted BODIPY compounds were successfully synthesized and characterized. The antioxidant, antidiabetic, antibiofilm, microbial cell viability, antimicrobial, antimicrobial photodynamic therapy, and DNA cleavage abilities of the BODIPY derivates were also tested. The highest antioxidant activity at 100 mg/L was 87.12% for BODIPY‐1, 85.61% for BODIPY‐2, and 92.78% for BODIPY‐3. The most effective inhibition of microbial cell viability was obtained for these BODIPY molecules at 100% at 50 and 100 mg/L. It was also observed that these BODIPY molecules exhibited excellent biofilm inhibition activities. The derivates were found to exhibit higher antibiofilm abilities against Staphylococcus aureus compared to Pseudomonas aeruginosa. When the antidiabetic effects of water‐soluble BODIPY compounds were examined, the highest effect was found to be 64.40% for BODIPY‐1 at 200 mg/L.