Radiolabeling, biological evaluation and molecular docking of delafloxacin: a novel methicillin-resistant Staphylococcus aureus infection radiotracer
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Labeling of delafloxacin with technetium-99m (99mTc) and its characterization in terms of in vitro stability and in vitro binding with methicillin-resistant Staphylococcus aureus (MRSA) were explored. Optimum amounts of reactants were 2.5 mg delafloxacin, 125 µg stannous chloride dihydrate and ~125 MBq pertechnetate. The 99mTc-delafloxacin was stable up to 6 h. Molecular modeling and docking studies showed that the complex will stabilize the DNA-topoisomerase IIA cleavage complex and inhibit strands separation. The in vivo evaluation showed highest specific accumulation in the live MRSA model (8 %) compared to other models. All gathered data supported the usefulness of 99mTc-delafloxacin as a MRSA radiotracer.
KeywordsDelafloxacin Technetium-99m Methicillin-resistant Staphylococcus aureus infection Septic inflammation Molecular modeling and docking
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