Actoprotective properties of 7'-((3-thio-4-methyl-4H-1,2,4-triazole-5-yl)methyl)theophylline derivatives
DOI:
https://doi.org/10.14739/2310-1210.2016.3.76926Keywords:
1, 2, 4-triazoles, Theophylline, Actoprotective PropertiesAbstract
The aim of this work was the study of actoprotective activity of compounds, which combine sintons of 1,2,4-triazole-3-thiol and theophylline.
Materials and methods. The first time synthesized 7'-((3-thio-4-phenyl-4H-1,2,4-triazole-5-yl)methyl)theophylline derivatives have been used for the research. The systemic toxicity and the acute toxicity of the studied compounds have been performed by the rapid method of Prozorovskiy to determine the optimal conditions for dispensing substances. Experiments have been conducted on a group of white nonlinear rats, 159–221 g weight. During the study of actoprotective activity the method of forced immersion in water with a load of 10% by weight of the rats has been used. The substances were administered at a dose 1/10 of LD50, and the reference drug «Riboxin» at a dose of 100 mg/kg. The swim time was recorded in seconds. The control group of animals was used for comparison; these animals received saline solution intraperitoneally 20 minutes before immersion. The obtained results were statistically processed using the standard software package of Microsoft Office 2007 and «STATISTICA@ for Windows 6.0».
Results. According to the results of conducted researches it has been established that the most active compound among the studied was 7'-((5-(2-hydroxyethylthio)-4-phenyl-4H-1,2,4-triazole-3-yl)methyl)theophylline, which increased the duration of swimming by 14.31% comparing to control group, whereas the reference drug increased it by 20.57%. It has been established that 2-((5-((theophylline-7'-yl)methyl)-4-phenyl-4H-1,2,4-triazol-3-yl)thio)-N'-(3,4-difluorobenzylidene)acetohydrazide also increases the duration of swimming.
Conclusion. The study of actoprotective activity of 13 first time synthesized compounds has been conducted. 7'-((5-(2-Hydroxyethylthio)-4-phenyl-4H-1,2,4-triazole-3-yl)methyl)theophylline has been detected as the most active compound among the studied ones.
References
Bobkov, Yu. G., Vinogradov, V. I., Katkov, V. F., Losev, S. S., & Smirnov, A. V. (1984). Farmakologicheskaya korrekciya utomleniya. [Pharmacological correction of fatigue]. Moscow: Meditsin. [in Russian].
Garev, A. I., Marysheva, V. V., & Shabanov, P. D. (2010) Aktoprotektornoe dejstvie antigipoksantov tiazoloindol'nogo ryada [The actoprotective action of thiazoloindole antihypoxic agents]. E'ksperimental'naya i klinicheskaya farmakologiya, 73(2), 25–30. [in Russian].
Lapach, S. N, Chubenko, A. V., Babich, P. N. (2001). Statisticheskiye metody v mediko-biologicheskikh issledovaniyakh s vnedreniyem Excel [Statistical methods in biomedical research with the introduction of Excel]. Kiev: Morion, 408. [in Ukrainian].
Stefanov, A. V. (Eds) (2001). Metodychní vkazívki po do klíníchnomu vyvchenniu líkars'kykh zasobív. [Guidelines for the clinical study of drugs]. Kyiv. [in Ukrainian].
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].
Andronati, S. A., Soboleva, S. G., Zamkovaya, A. V., Karaseva, T. L., Rakipov, I. M., & Cimbal D. I. (2016). Proizvodnye [(N-aril)piperazinil]butilpirimidinov, obladayushchie nejrotropnymi i aktoprotektornymi svojstvami. [[(N-aryl)piperazinil]buthylpyrimidine derivatives with neurotropic and actoprotective properties]. Zhurnal orhanichnoii ta farmatsevtychnoii khimii, 1(53), 53–60. [in Ukrainian].
Rebrova, O. Yu. (2002). Statisticheskij analiz medicinskikh dannykh. Primeneniye paketa prikladnykh programm STATISTICA [Statistical analysis of medical data. The use of STATISTICA software package]. Moscow: MediaSfera. [in Russian].
Ruda, N. V., Stepanyuk, H. Y., & Drachuk, O. P. (2013). Aktoprotektornoe deystvie kalievoy soli 2-glitsino-3-hlor-1,4-naftohinona v usloviyakh e'ksperimentalnoj gipokinezii [Actprotective activity of potassium salt of 2-glicino-3-chlor-1,4-naphthoquinone in experimental hypokinetic conditions]. Curierul medical, 1(56), 26–29. [in Moldova].
Soboleva, S. G., Andronati, S. A., Karaseva, T. I., Kostenko, E. A. (2013). Sintez i aktoprotektornye svojstva proizvodnykh 2-(β-morfolino)e'tilmerkapto-1,6-digidropirimidina [Synthesis and actoprotective properties of 2-(β-morpholino)-ethylmercapto-1,6-dihydropirimidine derivatives]. Dopovіdі Natsіonalnoi akademіi nauk, 2, 119–124. [in Ukrainian].
Stepaniuk, H. Í., Pochelova, O. V., Chornoívan, N. H., Denysiuk, O. M. (2012). Kharakterystyka aktoprotektornoii dii pokhidnykh (3-R-okso-2N-[1,2,4]-triazyno-[2,2-s]-khinazolin-6-il) karbonovykh kyslot za riznykh temperaturnykh rezhymiv [Сharacteristics of actoprotective actions of (3-R-oxo-2H-[1,2,4]-triazino-[2,2-c]-quinazolin-6-yl) carboxylic acid derivatives at different temperature conditions]. Farmakolohiia ta likarska toksykolohiia, 19, 132–134. [in Ukrainian].
Downloads
How to Cite
Issue
Section
License
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)
