α-Umpolung/Michael Addition/Quaternization Tandem Reaction to provide α-Imido-β-phosphonium Propanoates with Broad Spectrum of Biological Activity.

This paper has been supported by the Kazan Federal University Strategic Academic Leadership Program ('PRIORITY-2030'). HRMS data were obtained in the CSF-SAC FRC KSC RAS by support of the State Assignment of the Federal Research Center "Kazan Scientific Center", Russian Academy of Sciences. A.

New substituted 1,2,3-triazoles for ratiometric recognition to Fe ions.

Two novel click derived sensory systems for different derivatives connected via a triazole linkage have been developed as a component of a chemosensor with sensitive towards Fe ions. The 1-octyl-4-carboxyl-1,2,3-triazole (TR1) system demonstrated sensitivity to calcium ion. The 1,3-bis(4-hydroxycarbamoyl-1,2,3-triazol-1-yl)xylylene (TR2) system was shown to possess a preferential detection capability as a colorimetric probe for Fe ions by exhibiting an obvious pH-dependent color change from colorless to pink.

Conjugates of nucleobases with triazole-hydroxamic acids for the reactivation of acetylcholinesterase and treatment of delayed neurodegeneration induced by organophosphate poisoning.

A series of new uncharged conjugates of adenine, 3,6-dimetyl-, 1,6-dimethyl- and 6-methyluracil with 1,2,4-triazole-3-hydroxamic and 1,2,3-triazole-4-hydroxamic acid moieties were synthesized and studied as reactivators of organophosphate-inhibited cholinesterase. It is shown that triazole-hydroxamic acids can reactivate acetylcholinesterase (AChE) inhibited by paraoxon (POX) in vitro, offering reactivation constants comparable to those of pralidoxime (2-PAM). However, in contrast to 2-PAM, triazole-hydroxamic acids demonstrated the ability to reactivate AChE in the brain of rats poisoned with POX.

Thymine-Modified Nanocarrier for Doxorubicin Delivery in Glioblastoma Cells.

Brain tumor glioblastoma is one of the worst types of cancer. The blood-brain barrier prevents drugs from reaching brain cells and shields glioblastoma from treatment. The creation of nanocarriers to improve drug delivery and internalization effectiveness may be the solution to this issue.