Actoprotective activity of 5-(2-bromophenyl)-4-amino-4H-1,2,4-triazole-3-thione and its S-derivatives
Keywords:Riboxin, Anti-Fatigue Activities, 1, 2, 4-triazole, Weight Loaded Forced Swimming Test
Aim. The paper shows the actoprotective (anti-fatigue), activity of 1,2,4-triazole derivatives.
Methods and results. The analysis of action was conducted for the synthesized 2-(5-(2-bromphenyl)-4-amino-4H-1,2,4-triazol-3-ylthio) acetic acid salts. We have revealed some patterns regarding to the chemical structure and pharmacological action of the test substances.
Thus, in the research we have found that the most active compound among the studied was morpholinium 2-(5-(2-bromphenyl)-4-amino-4H-1,2,4-triazol-3-ylthio) acetate (3j), which increases the duration of rats (forced swimming with the load) as compared with the control group at 77,17% (p˂0,05), while the reference drug increases the rate at 24,16% (p˂0,05).
We have noted the compound 3i which exceed its activity comparing to Riboxinum at 23,2%, with increased endurance during the animals forced swimming test to 47,36% (p˂0,05).
Conclusions. It is marked that the parent thione 1a and its derivative of 2-(5-(2-bromophenyl)-4-amino-4H-1,2,4-triazol-3-ylthio) acetic acid salt 2a and 3d, 3e, 3f have no actoprotective properties in their application.
After analyzing the data of experimental studies some laws concerning the chemical structure and pharmacological action of the test substance have been established.
Arlashchenko, N. I., Kolodin, A. B., & Meshkov, H. A. (1994) Antigipoksantnoe i aktoprotektornoe dejstvie paraaminobenzojnoj kisloty [Antihypoxic and actoprotective action of para-aminobenzoic acid]. Antigipoksanty i aktoprotektory: itogi i perspektivy; Proceedings of the Russian Conference, (Issue 2), (p. 229). Saint Petersburg. [in Russian].
Bobkov, Yu. G., Vinogradov, V. I., Katkov, V. F., Losev, S. S., & Smirnov, A. V. (1984) Farmakologicheskaya korrekciya utomleniya [Pharmacological correction of fatigue]. Moscow: Medicina. [in Russian].
Ganapol'skij, V. P. (2008) Razrabotka i izucheniye novykh meteoadaptagenov (Avtoref. dis… dokt. med. nauk) [Development and study of new genes meteoadaptogens. Dr. med. sci. diss.] Saint Petersburg. [in Russian].
Knysh, Ye. G. (1987) Sintez, fiziko-khimicheskiye i biologicheskiye svojstva N- i Szameshchennykh 1,2,4-triazola. (Dis… dokt. farm. nauk). [Synthesis, physicochemical and biological properties of N- and S substituted 1,2,4-triazole. Dr. farm. sci. diss.] Kharkiv. [in Ukrainian].
Lapach, S. N., Chubenko, A. V., & Babich, P. N. (2001) Statisticheskie metody v mediko-biologicheskikh issledovaniyakh s vnedreniyem Excel [Statistical methods in biomedical research with the introduction of Excel]. Kyiv: Morion. [in Ukrainian].
Mashkovskij, M. D. (2005) Lekarstvennyye sredstva [Drugs]. Moscow: Novaya volna. [in Russian].
Stefanov, A. V. (Ed) (2001) Metodychni vkazivky po doklinichnomu vyvchenniu likarskykh zasobiv [Guidance on pre-clinical study of drugs]. Kyiv [in Ukrainian]
Novikov, B. C., Cheprasov, V. Yu., Kolosov, I. A., et al. (1994) E′kstremal'naya proverka aktoprotektornoj aktivnosti peptidnykh bioregulyatorov [Extreme check hepatoprotective activity of peptide bioregulators]. Antigipoksanty i aktoprotektory: itogi i perspektivy. Proceedings of the Russian Conference, (Issue 3), (p. 271). Saint Petersburg. [in Russian].
Prozorovskii, V. B. (2007) Statisticheskaya obrabotka rezul'tatov farmakologicheskikh issledovanij [Statistic processing of data of pharmacological investigations]. Psikhofarmakologiya i biologicheskaya narkologiya, 7(3–4), 2090–2120. [in Russian].
Rebrova, O. Yu. (2002) Statisticheskij analiz medicinskikh dannykh. Primeneniye paketa prikladnykh programm STATISTICA [Statistical analysis of medical data. The use of the application package STATISTICA]. Moscow: MediaSfera. [in Russian].
Stepaniuk, H. I., Pochelova, O. V., & Chornoivan, N. H., et al. (2012) Skryninh aktoprotektornoi dii v riadu pokhidnykh (3-R-okso-2N- [1,2,4]-triazyno- [2,2-s]-khinazolin- 6-il)karbonovykh kyslot [Screening Actoprotective action in a number of derivatives (3-R-oxo-2H [1,2,4] -triazyno- [2,2-c] -hinazolin- 6-yl) carboxylic acids]. Biomedical and Biosocial Antropology, 19, 132–134.
Tomchin, A. B., & Marysheva, B. B. (1994) Proizvodnyye tiomocheviny i tiosemikarbazida v kachestve antigipoksantov i aktoprotektorov [Derivatives of thiourea and thiosemicarbazide as antihypoxants and actoprotector] Antigipoksanty i aktoprotektory. Proceedings of the Scientific Conference, (Issue 2), (p. 99). Saint Petersburg. [in Russian].
Oleynik, S. A., Gunina, L. M., Sejfulla, R. D. (2010) Farmakologiya sporta [Pharmacology sports]. Kyiv: Olimpijskaya literature. [in Ukrainian].
Shabanov, P. D., & Lebedev, A. A. (2008) E′kspressiya mRNK kortikoliberina i vazopressina v gipotalamuse i mindaline krys pri vvedenii deksametazona i psikhoaktivnykh veshchestv [Expression of NK kortykoliberyn and vasopressin in the hypothalamus and amygdala in rats when administered dexamethasone and substance]. Psikhofarmakologiya i biologicheskaya narkologiya, 8(1–2), 2383. [in Russian].
How to Cite
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)