One of the promising areas in the creation of bioregulators is the modeling of compounds that combine several pharmacophores. The design of new highly efficient and low-toxic cytoprotectors is largely based on the deriva-tives of nitrogen-containing heterocycles, and quinoline plays a significant role among these compounds.
The researchers evaluated the toxicity of the tested com-pounds in silico, in vitro, and in vivo, which allowed deter-mining several factors that affect the level of toxic action of 4-thioquinoline derivatives and the direction of non-toxic substances in this sequence.
The studied 4-thioquinolines showed a moderate antiradical action in the experiment, inferior to the reference antioxi-dant Acetylcysteine. The most active compounds are 7-chloro-4-thioquinoline derivatives with propanoic acid residues in the 4th position. 2-(7-chloroquinolin-4-ylthio)propanoic acid and sodium salt of 2-amino-3-((7-chloroquinolin-4-yl)thio)propanoic acid showed the most promising results and their antioxidant action was higher than Tiotriazolin (the comparator) by 27 % and 41 %, re-spectively.
The studied compounds showed a protective effect under H2O2-induced oxidative stress against male sperm accord-ing to the main indicators of sperm fertility. It was found that the compounds with residues of succinic acid, cys-teamine, or cysteine in the molecule structure are not infe-rior to reference drugs. On average, 2-((7-chloroquinolin-4-yl)thio)succinic acid and 2-((quinolin-4-yl)thio)ethanaminedihydrochloride exceeded the comparison drug Acetylcys-teine and were on a par with the effect of Ascorbic acid.
Title
Design, synthesis and biological activity оf the 4-thioquinoline derivatives
Design, synthesis and biological activity оf the 4-thioquinoline derivatives / A. Bohdan, Y. Romanenko, M. Zavhorodnii and others // Chemistry & chemical technology. – 2023. - Vol. 17. - No. 4. - Р. 774-785.
