Publications by authors named "Garret P Textor"
Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of new anticoagulant agents. We previously reported the imidazo[1,5-c]imidazol-3-one derivative 1 as a potent and orally active FXa inhibitor. However, it was found that 1 predominantly undergoes hydrolysis upon incubation with human liver microsomes, and the human specific metabolic pathway made it difficult to predict the human pharmacokinetics.
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- GSK-3beta inhibition is seen as a potential treatment for Alzheimer's disease, with previous research identifying 1,3,4-oxadiazole derivatives as effective inhibitors but facing pharmacokinetic challenges.
- Researchers improved these derivatives by reducing their molecular weight and lipophilicity, leading to the development of sulfinyl group-containing compounds (S)-9b and (S)-9c, which exhibited good pharmacokinetic properties and selective inhibition of GSK-3beta.
- Both (S)-9b and (S)-9c, when administered orally to mice, effectively reduced tau hyperphosphorylation in the brain, indicating their potential therapeutic benefits.