Design, synthesis and multitarget evaluation of cyclopropyl-appended thiohydantoin derivatives as dual cholinesterase and COX inhibitors with antioxidant activity: a combined experimental and computational study
Together with their dual cholinesterase inhibitory activities, compounds 6a and 6c represent promising multifunctional in vitro lead candidates for further development against neurodegenerative disorders associated with neurodegenerative disorders associated with neuroinflammation and oxidative stress.
Alzheimer's disease remains one of the leading causes of dementia, and the development of novel cholinesterase inhibitors continues to attract considerable interest for symptomatic treatment. In this study, a series of five novel 5-(benzylthio)-1,3,4-thiadiazole derivatives bearing different nitrogen-containing substit...
Mahmut Gozelle, Burcu Kılıç· Journal of Gazi university h...· 0 citations
This work employed regioselective Williamson O-alkylation to semi-synthesize three novel α-M alkylamine derivatives, enabling tunable mono- and disubstitution, highlighting the potential of tunable α-M derivatives as promising anti-AD candidates.
A new series of quinoline-diphenylpyrazole hybrids were rationally designed, synthesized, and biologically evaluated as potential EGFR/VEGFR-2/COX-2 inhibitors, supporting the proposed hybrid design strategy.
Abdelrahman Hamdi, Mohamed R. Elnagar, M. Hussein et al.· Bioorganic chemistry (Print)· 0 citations
The rational design, synthesis, and biological evaluation of a new series of indole-piperazine based α-ketoamide moiety MD08 identify MD08 as a promising dual aggregation modulator for AD, warranting further preclinical investigation.
Bhanuranjan Das, Anurag T. K. Baidya, Deepak Chouhan et al.· European journal of medicina...· 0 citations
Compound 17v represents a promising lead compound for anti-Alzheimer's therapy and may possess multi-target neuroprotective potential and a favorable preliminary safety profile, supporting its further investigation as a potential therapeutic candidate for Alzheimer’s disease.
Yi-Xuan Wang, Shi-Hao Qin, Qiang Liu et al.· Medicinal Chemistry Research· 0 citations