Anti-tuberculosis activity research of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol

Authors

  • A. A. Safonov Zaporizhzhia State Medical University, Ukraine,
  • V. V. Zazharskyi Dnipro State Agrarian and Economic University, Ukraine,

DOI:

https://doi.org/10.14739/2409-2932.2019.3.184178

Keywords:

1, 2, 4-triazole, anti-tuberculosis activity, heterocyclic compounds

Abstract

 

Introduction. 1,2,4-Triazole derivatives have already proven themselves to be compounds with low toxicity and high antimicrobial, antifungal, antiviral, hepatoprotective activity.

The aim of work is to research the anti-tuberculosis activity of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazoles-3-thiol on the bacteria strain M. bovis.

Materials and methods. At the beginning of the experiment, the effect of the drug concentration and the pH of the medium on the growth rate of the culture at 37 °C was detected. M. bovis 100 passage was selected for this purpose, which was cultured at 37 °C with 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol at the indicated concentrations in a thermostat for 3 months on medium with pH 6.5 (ten test tubes with each medicine concentration) and pH 7.1 (ten test tubes with each medicine concentration). M. bovis 100 passage was used as a control without the addition of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol to the medium.

Results. The results of the experiment show that the effect of the drug at different concentrations on the medium with a pH 6.5 same with pH 7.1. Growth of pathogenic strain M. bovis 100 passages throughout the observation period (90 days) have been absence for all of the test (0.1 %, 0.5 % and 1.0 %) concentrations of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazoles-3-thiol.

Conclusion. It can be concluded that 0.1 %, 0.5 % and 1.0 % concentration of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol influence on the culture properties pathogenic strain M. bovis, which cultured on the medium with pH 6.5 and pH 7.1 at 37 °C, while holding back growth, having a tuberculostatic effect.

References

El-wahab, H., Abdel-Rahman H. M., Gamal-Eldin, S. A., & El-Gendy, M. A. (2011). Synthesis, biological evaluation and molecular modeling study of substituted 1,2,4-triazole-3-acetic acid derivatives. Der Pharma Chemica, 3(6), 540-552.

Kaplaushenko, A. H., Sameliuk, Yu. H., & Kucheriavyi, Yu. M. et al. (2016). Praktychne znachennia ta zastosuvannia pokhidnykh 1,2,4-triazolu [Practical value and application of derivatives of 1,2,4-triazole]. Zaporizhzhia. [in Ukrainian].

Hulina, Yu. S., & Kaplaushenko, А. G. (2018). Synthesis, physical and chemical properties of 5-((1Н-tetrazole-1-yl)methyl)-4-R-4Н-1,2,4-triazole-3-thiols and their chemical transformations. Biopharmaceutical jornal, 1(10), 26-30.

Rud, A., Kaplaushenko, A., & Yurchenko, I. (2018). Synthesis, physical and chemical properties of 2-((5-(hydroxy(phenyl)methyl)-4R-4H-1,2,4-triazole-3-yl)thio)acetic acids and its salts. Zaporozhye medical journal, 20(1), 105-109. doi: 10.14739/2310-1210.2018.1.122126

Wu, J., Yin, L., Liu, Y., Zhang, H., Xie, Y., & Wang, R., et al. (2019). Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout. Bioorganic & Medicinal Chemistry Letters, 29(3), 383-388. doi: 10.1016/j.bmcl.2018.12.036

Hassan, A., Mohamed, N., Aly, A., Tawfeek, H., Bräse, S., & Nieger, M. (2019). Eschenmoser‐Coupling Reaction Furnishes Diazenyl‐1,2,4‐triazole‐5(4H)‐thione Derivatives. Chemistry Select, 4(2), 465-468. doi: 10.1002/slct.201802870

Moreno-Fuquen, R., Arango-Daraviña, K., Becerra, D., Castillo, J., Kennedy, A., & Macías, M. (2019). Catalyst- and solvent-free synthesis of 2-fluoro-N-(3-methylsulfanyl-1H-1,2,4-triazol-5-yl)benzamide through a microwave-assisted Fries rearrangement: X-ray structural and theoretical studies. Acta Crystallographica Section C Structural Chemistry, 75(3), 359-371. doi: 10.1107/s2053229619002572

Hulina, Yu., & Kaplaushenko, A. (2016). Syntez i fizyko-khimichni vlastyvosti 2-(5-(1N-tetrazol-1-ilmetyl)-4-R-4N-1,2,4-triazol-3-iltio)-atsetatnykh (propanovykh), 2-, 4-(5-(1N-tetrazol-1-ilmetyl)-4-fenil-4N-1,2,4-triazol-3-iltiometyl)-benzoinykh kyslot ta yikh solei [Synthesis and physical-chemical properties of 2-(5-(1Н-tetrazol-1-ylmethyl)-4-R-4Н-1,2,4-triazol-3-yltio)-acetic (propanoic), 2-, 4-(5-(1Н-tetrazol-1- ylmethyl)-4-phenyl-4Н-1,2,4-triazol-3- yltiometil)-benzoic acids and their salts]. Current issues in pharmacy and medicine: science and practice, 2(21), 32-37. doi: 10.14739/2409-2932.2016.2.71115 [in Ukrainian].

Tang, Y., Yu, F., Huang, L., & Hu, Z. (2019). The changes of antifungal susceptibilities caused by the phenotypic switching of Candida species in 229 patients with vulvovaginal candidiasis. Journal Of Clinical Laboratory Analysis, 33(1), e22644. doi: 10.1002/jcla.22644

Lindberg, E., Hammarström, H., Ataollahy, N., & Kondori, N. (2019). Species distribution and antifungal drug susceptibilities of yeasts isolated from the blood samples of patients with candidemia. Scientific Reports, 9(1):3838. doi: 10.1038/s41598-019-40280-8

Gautier-Veyret, E., Truffot, A., Bailly, S., Fonrose, X., Thiebaut-Bertrand, A., & Tonini, J., et al. (2019). Inflammation is a potential risk factor of voriconazole overdose in hematological patients. Fundamental and Clinical Pharmacology, 33(2), 232-238. doi: 10.1111/fcp.12422

Johnston, S., Puhalla, S., Wheatley, D., Ring, A., Barry, P., & Holcombe, C. et al. (2019). Randomized phase II study evaluating palbociclib in addition to letrozole as neoadjuvant therapy in estrogen receptor – positive early breast cancer: PALLET trial. Journal Of Clinical Oncology, 37(3), 178-189. doi: 10.1200/jco.18.01624

Mitwally, M., & Casper, R. (2001). Use of an aromatase inhibitor for induction of ovulation in patients with an inadequate response to clomiphene citrate. Fertility And Sterility, 75(2), 305-309. doi: 10.1016/s0015-0282(00)01705-2

Rud, A. M., Kaplaushenko, A. G., Pruglo, Ye. S., & Frolova, Yu. S. (2018). Vstanovlennia pokaznykiv diuretychnoi dii (3-tio-4-R-4N-1,2,4-triazol-5-il)(fenil) metanoliv ta yikh pokhidnykh [Establishment of diuretic activity indicators for (3-thio-4-R-4-H-1,2,4-triazole-5-yl)(phenyl)methanols and their derivatives]. Current issues in pharmacy and medicine: science and practice, 2, 215-219. doi: 10.14739/2409-2932.2018.2.134004 [in Ukrainian].

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1.
Safonov AA, Zazharskyi VV. Anti-tuberculosis activity research of 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol. Current issues in pharmacy and medicine: science and practice [Internet]. 2019Nov.21 [cited 2024Jul.21];(3). Available from: http://pharmed.zsmu.edu.ua/article/view/184178

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