Registration Number
0222U003604,
0116U005355
, R & D reports
Title
The pharmacological actuvity of new derivatuves of five-and six-membered heterociclic and grugs of natural origin and marketing studies of the pharmaceutical market of Ukraine
popup.stage_title
Head
Білай Іван Михайлович,
Registration Date
07-05-2022
Organization
Zaporizhzhya State Medical University
popup.description2
According to the results of acute toxicity study of 37 compounds synthesized for the first time among azaheterocycle derivatives, it was found that all selected compounds with LD50 (566 and 3340 mg / kg) are low-toxic, practically non-toxic or relatively harmless according to K.K. Sidorova. Analysis of the dependence "chemical structure - pharmacological activity" among the 30 studied substances showed that the presence and severity of hypoglycemic activity depends on the functional substitutes on the C7 position of the nucleus of 3-methylxanthine.
A significant increase in these activities was observed with the introduction of position 7 of the original 3-benzyl-8-methylxanthine n-propyl acetate residue, which is shown in the example of compound 70. The most pronounced hypoglycemic activity was manifested using 3-benzyl-8-methylxanthinyl-7-acetate acids in doses of 1/5 and 1/10 of LD50 and reduced glucose better than the comparison drug metformin (66.67% and 65.74%, respectively). According to the results of the experiment, the substance PK-282 showed the highest analgesic activity, which exceeded analgin. The obtained data indicate the presence of analgesic activity in a number of derivatives of 1,2,4-triazole, which creates the preconditions for further in-depth specific study of the most active substances. In the process of analysis of further results of preclinical research it is necessary to evaluate the effectiveness, safety of the test compound and the feasibility of its use in practical medicine.
Product Description
popup.authors
Ahibailov Maksym Viacheslavovych
Mazulin Oleksandr Vladylenovych
Mihayluk Evgeniy Olehovich
Popova Yana Vasylivna
Pruhlo Yevhen Serhiiovych
Raikova Tetiana Semenivna
Khilkovets Anastasiia Valeriivna
popup.nrat_date
2022-05-07
