376. Synthesis, hemorheological and antifibrotic activity of newly synthesized 3-acetyl-2,4,6-trimethylpyridine derivatives
Zarina Shulgau, Alena Stalinskaya, Shynggys Sergazy, Aigerim Zhulikeyeva, Yevgeniy Kamyshanskiy, Alexander Gulyayev, Yerlan Ramankulov and Ivan Kulakov; Arabian Journal of Chemistry (2023); DOI: 10.1016/j.arabjc.2023.104821 (open access)
Pyridine derivatives still attract the attention of many researchers for their comprehensive biological research, possible promotion to the pharmaceutical market in order to be used as effective drugs. In this article, based on the well-known and fairly accessible in terms of laboratory synthesis of the 3-acetyl derivative of collidine, we carried out several simple chemical modifications to obtain new collidine derivatives not previously described. The structure of the synthesized compounds was confirmed by 1H- and 13C-NMR spectroscopy. A biological screening of the synthesized compounds for hemorheological activity was carried out on an in vitro blood hyperviscosity model. It was shown that pronounced hemorheological activity was established for compounds 3, 4 and 5. Compound 4 also showed a pronounced antifibrotic effect in an experimental model of pulmonary fibrosis induced by intratracheal administration of bleomycin to rats. In an experimental model of pulmonary fibrosis in rats, the formation of a hyperviscosity syndrome was also observed, and blood viscosity decreased when compound 4 was administered to animals.