has been studied and the formation of acrolein as a product confirmed by gas chromatography-mass spectrometry. Oxi dation of 4-methylcyclophosphamide generates methyl vinyl ketone. This is interpreted to indicate that the acrolein and methyl vinyl ketone arise from oxidation of position 4 of the ring of cyclophosphamide. The Fenton oxidation of both cyclophosphamide and 4-methylcylophosphamide ...

Topical corticosteroids are effective in reducing anterior segment inflammation but are associated with adverse drug reactions (ADRs) including elevation of intraocular pressure (IOP) and cataract formation. Retrometabolic drug design has advanced the development of new corticosteroids with improved therapeutic indices. Engineered from prednisolone, loteprednol etabonate (LE) has a 17α-chlorome...

In the Baylis-Hillman reaction of aryl aldehydes with phenyl vinyl ketone we have observed exclusive formation of diadducts 4, and that the yields of diadduct can reach 80% with increasing amounts of phenyl vinyl ketone. On the other hand, for phenyl acrylate and phenyl thioacrylate, only the normal Baylis-Hillman adduct was obtained. The effects of substituents were also examined and a plausib...

Mechanistic studies of the enolization of 2-methylcyclohexanone mediated by lithium hexamethyldisilazide (LiHMDS; TMS2NLi) in toluene and toluene/amine mixtures are described. NMR spectroscopic studies of LiHMDS/ketone mixtures in toluene reveal the ketone-complexed cyclic dimer (TMS2NLi)2(ketone). Rate studies using in situ IR spectroscopy show the enolization proceeds via a dimer-based transi...

Carboxylesterases are important enzymes responsible for the hydrolysis and metabolism of numerous pharmaceuticals and xenobiotics. These enzymes are potently inhibited by trifluoromethyl ketone containing (TFK) inhibitors. We demonstrated that the ketone hydration state was affected by the surrounding chemical moieties and was related to inhibitor potency, with inhibitors that favored the gem-d...

Background. The acute ingestion of ketone body supplements can improve exercise responses such as oxygen consumption and blood lactate. Additionally, ketone body supplements show increases in circulating βhb concentration, matching those of someone in a state of nutritional ketosis. Studies testing ketone body supplements have reported different results in exercise response and varying gastroin...