#PAGE_PARAMS# #ADS_HEAD_SCRIPTS# #MICRODATA#

Štúdium hypoglykemickej aktivity kyselín a solí obsahujúcich 1,2,4-triazol


Authors: Dmytro Dovbnia;  Yuliia Frolova;  Andrii Kaplaushenko
Published in: Čes. slov. Farm., 2023; 72, 113-124
Category: Original Article
doi: https://doi.org/10.5817/CSF2023-3-113

Overview

Článok prezentuje výsledky štúdie hypoglykemických vlastností medzi 1,2,4-triazolovými derivátmi syntetizovanými na Katedre fyzikálnej a koloidnej chémie Štátnej lekárskej univerzity v Zaporizhzhia. V súčasnosti má veľké množstvo ľudí sedavý spôsob života, aj väčšina ich stravy obsahuje často používané produkty, ktoré zvyšujú hladinu glukózy v krvi, čo môže vyvolať rozvoj závažných ochorení. Preto do dnešného dňa zostáva vytvorenie liekov, ktoré vykazujú hypoglykemickú aktivitu a majú nízku úroveň toxicity, naliehavou úlohou pre lekárne. V prvej fáze nášho výskumu bola vykonaná predpoveď akútnej toxicity. Hypoglykemická aktivita syntetizovaných zlúčenín bola hodnotená vykonaním intraperitoneálneho glukózového tolerančného testu (IPGTT) so zmenou koncentrácie glukózy v krvi zvieraťa po jeho jednorazovom intraperitoneálnom podaní vo forme 40 % roztoku v dávke 2 g/kg telesnej hmotnosti potkana. Zlúčeniny (38) rôznych tried boli študované na hypoglykemickú aktivitu. 2-{5-[(3,4-dimetoxyfenyl)-3H-1,2,4-triazol-3-yl]sulfanyl}acetát zinočnatý (3.18) vykazoval najvyššiu účinnosť z hľadiska schopnosti znižovať krv hladiny glukózy, a to o 27,3 % (približne 1,3-krát).

Klíčová slova:

1,2,4-triazol – hypoglykemická aktivita – intraperitoneálny glukózový tolerančný test


Sources

1. Samelyuk Yu. H. Synthesis and study of biologically active derivatives of 1,2,4-triazole-3-thione containing methoxyphenyl substituents. PhD thesis: 15.00.02. Zaporizhzhia 2016; 235 [in Ukrainian].

2. Dovbnia D. V., Kaplaushenko A. H., Frolova Yu. S. Synthesis and transformation in the series of 2-((5-(2,4- and 3,4-dimethoxyphenyl)-3H-1,2,4-triazole-3-yl)thio)acetic acids. Curr. Issues Pharm. Med. Sci. 2021; 14(1), 12–16.

3. Dovbnia D. V., Kaplaushenko A. H., Korzhova A. S. Synthesis and alkylation of 5-aryl-1,2-dihydro-3H-1,2,4-triazole-3-thions. J. Org. Chem. 2021; 2, 53–59.

4. Hulina Y. S., Kaplaushenko A. G. Synthesis, physical and chemical properties of 5-((1H-tetrazole-1-yl)methyl)-4-R-4H-1,2,4-triazole-3-thiols and their chemical transformations. Russ. J. Biopharm. 2018; 10(1), 26–30.

5. Kaplaushenko A. H. Synthesis methods and biological activity of 1,2,4-triazol-3-thions. Ukraine Вiofarmatceutical Journal 2009; 4, 48–53 [in Ukrainian].

6. Kaplaushenko A. H. Chemical properties of amino and thio-substituted 1,2,4-triazoles. Current issues in pharmacy and medicine: science and practice 2015; 1, 101–106 [in Ukrainian].

7. Frolova, Y., Kaplaushenko, A., Nagornaya, N. Design, synthesis, antimicrobial and antifungal activities of new 1,2,4-triazole derivatives containing 1H-tetrazole moiety. Ankara Universitesi Eczacilik Fakultesi Dergisi 2020; 44(1), 70–88.

8. Gotsulya A. S. Synthesis and antiradical activity of alkyl derivatives of 5-(5-methyl-1H-pyrazol-3-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol. J. Fac. Pharm. Ankara 2020; 44(2), 211–219.

9. Sameliuk Y., Kaplaushenko T., Al Zedan F. 1,2,4-triazole derivatives in medicine and pharmacy and application prospects. J. Fac. Pharm. Ankara 2021; 45(3), 598–614.

10. Shcherbyna R. Microwave-assisted synthesis of some new derivatives of 4-substituted-3-(morpholinometh-yl)-4H-1,2,4-triazole-5-thioles. J. Fac. Pharm. Ankara 2019; 43(3), 220–229.

11. Shcherbyna R., Parchenko V., Varynskyi B., Kaplaushenko A. The development of HPLC-DAD method for determination of active pharmaceutical ingredient in the potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio)acetate substance. Curr. Issues Pharm. Med. 2019; 32(1), 5–9.

12. Shcherbyna R, Parchenko V, Martynyshyn V, Hunchak V. Evaluation of acute and subacute toxicity of oil liniment based on 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazol-3-yl)methyl)morpholine. J. Fac. Pharm. Ankara 2018; 42(1), 43–52.

13. Samelyuk Yu. G., Kaplaushenko A. H. Synthesis of 3-alkylthio(sulfo)-1,2,4-triazoles, containing methoxyphenyl substituents at C5 atoms, their antipyretic activity, propensity to adsorption and acute toxicity. J. Chem. Pharm. Res. 2014; 6(5), 1117–1121.

14. Safonov A., Nevmyvaka A., Panasenko O., Knysh Ye. Microwave synthesis of 3- and 4-substituted-5-((3-phenylpropyl) thio)-4H-1,2,4-triazoles. J. Fac. Pharm. Ankara 2021; 45(3), 457–466.

15. Safonov A. Microwave synthesis of new 3-(alkylthio)-5-(thiophen2-ylmethyl)-1,2,4-triazol-4-amines. J. Fac. Pharm. Ankara 2020; 44(1), 89–98.

16. Web-service GUSAR on-line, http://www.way2drug.com/gusar/acutoxpredict.html

17. Dovbnya D., Kaplaushenko A., Frolova Yu., Pruglo E. Synthesis and antioxidant properties of new (2,4- and 3,4-dimethoxyphenyl)-1,2,4-triazoles. Pharmacia 2022; 69(1), 135–142.

18. Pretsch E., Buhlmann P., Badertscher M. Structure determination of organic compounds. Springer Berlin Heidelberg: Enlarg edition 2010.

19. Swapnil S., Swapnil D. Handbook of acute oral toxicity testing method. LAP LAMBERT Academic publishing 2011.

20. Reblova Z. Effect of temperature on the antioxidant activity of phenolic acids. Czech J. Food Sci. 2016; 30, 171–175.

21. Trudu F., Amato F., Vaňhara P. Coordination compounds in cancer: Past, present and perspectives. Journal of Applied Biomedicine 2015; 2, 79–103.

Labels
Pharmacy Clinical pharmacology
Topics Journals
Login
Forgotten password

Enter the email address that you registered with. We will send you instructions on how to set a new password.

Login

Don‘t have an account?  Create new account

#ADS_BOTTOM_SCRIPTS#