Anticoagulant activity of singlet oxygen released from a water soluble endoperoxide by thermal cycloreversion

Singlet oxygen generated by photosensitization has limited potential in vivo due to light attenuation in tissues. However, controlled chemical generation of this reactive oxygen species is likely to open new therapeutic spaces to explore. The fact that its activity is limited by the rate of cycloreversion reaction and the diffusion distance of the excited state molecular oxygen species, is a clear advantage, considering the serious side effects of off-target anticoagulants. In this work, we present novel 1,4-naphthalene endoperoxides as potential anti-coagulant agents due to thermal release of singlet oxygen.

Automated summary

Singlet oxygen generated by photosensitization has limited potential in vivo due to light attenuation in tissues, but controlled chemical generation of this reactive oxygen species may open up new therapeutic opportunities. The novel 1,4-naphthalene endoperoxides proposed as potential anti-coagulant agents due to thermal release of singlet oxygen offer advantages in terms of activity limitation and potential reduction of off-target anticoagulant side effects.