Methods of synthesis of 1,2,4-triazole derivatives with methoxyphenyl and study the spectrum of their pharmacological activity
Keywords:1,2,4-triazole derivatives, methoxyphenyl substituent, pharmacological activity
In today’s society, the work of a pharmaceutical worker is very respectful, because it is difficult to imagine the treatment of people without the use of drugs. As time passes, the number of diseases with their own characteristics only increases, so the creation of drugs of synthetic origin remains an actual task for scientists around the world. There are a large number of heterocyclic systems, the derivatives of which exhibit a wide range of pharmacological activities, namely, furan, pyrrole, pyrazole, pyridine, pyrimidine, purine, and many others. Particular attention is drawn to structures that have low toxicity. Undoubtedly, the initial heterocyclic substance must have several reactive centers in order to build the most effective pharmacophores.
Studies by scientists from around the world point to the prospect of using derivatives of the 1,2,4-triazole heterocyclic system as models for new biologically active substances.
The aim of the work was to summarize data on modern methods for the synthesis of 1,2,4-triazole derivatives, to determine the effect of a methoxyphenyl substituent on reactivity and changing the spectrum of pharmacological activity.
Materials and methods. In the work, we used such methods as analytical, information search, descriptive, generalization. The materials of the research were information from the professional literature on the methods of synthesis and study of the biological activity of 1,2,4-triazole derivatives with methoxyphenyl.
Results. A search, analysis, and generalization of information on the methods of synthesis and study of the biological activity of 1,2,4-triazole derivatives with methoxyphenyl were carried out. As a result of the studying available sources and implementation of scientific research, it was found that studies of 1,2,4-triazole derivatives with methoxyphenyl occupy an important place in the Ukrainian pharmaceutical industry, as they have a wide range of pharmacological activity. Also they show low rates of acute toxicity and are perspective to create new APIs on their base
Conclusions. Processing, analysis, systematization, comparison, and generalization of modern sources of information indicate a wide synthetic variability, a fairly wide range of biological activity, and low rates of acute toxicity of 1,2,4-triazole derivatives, with methoxyphenyl at the 5th position of the nucleus of this heterocycle and a wide range of their applications.
Fedotov, S. O., Hotsulia, A. S., Panasenko, O. I. (2022). Synthesis and properties of some 3-(5-(4-methoxyphenyl)pyrazol-3-yl)-6-R-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. Current issues in pharmacy and medicine: science and practice, 15(2), 117-122. https://doi.org/10.14739/2409-2932.2022.2.259227
Samelyuk, Y. G., & Kaplaushenko, A. G. (2013). Syntez, fizyko-khimichni ta biolohichni vlastyvosti 2-(5-(metoksyfenil)-1,2,4-triazol-3-tio) atsetatnykh kyslot ta yikh esteriv [Synthesis, physico-chemical and biological properties of 2-(5-(methoxyphenyl)-1,2,4-triazolo-3-thio)acetic acid and their esters]. Current issues in pharmacy and medicine: science and practice, (2), 125-128. [in Ukrainian].
Samelyuk, Yu. G., & Kaplaushenko, A. G. (2015). Hostra toksychnist 5-(2-, 3-, 4-metoksyfenil, (3,4,5-trymetoksyfenil)-)-1,2,4-triazol-3-tioniv ta yikh tiopokhidnykh Acute toxicity of 5-(2-, 3-, 4-methoxyphenyl, (3,4,5-trimethoxyphenyl)-)-1,2,4-triazole-3-thiones and its thioderivatives. Current issues in pharmacy and medicine: science and practice, (3), 57-60. [in Ukrainian]. https://dx.doi.org/10.14739/2409-2932.2015.3.52660
Biolohichna aktyvnist pokhidnykh 1,2,4-triazolu. Farmatsevtychnyi zhurnal
Kravchenko, T. V., Panasenko, O. I., & Knish E. G. (2016). Biolohichna aktyvnist pokhidnykh 1,2,4-triazolu [Biological activity of the derivatives 1,2,4-triazole]. Farmatsevtychnyi zhurnal, (5), 25-30. [in Ukrainian]. https://doi.org/10.32352/0367-3057.5.16.02
Shcherbyna, R. О., Panasenko, O. I., Knysh, Ye. H., & Varynskyy, B. О. (2014). Syntez i fizyko-khimichni vlastyvosti 2-((4-R-3-(morfolinometylen)-4H-1,2,4-triazol-5-il)tio)atsetatnykh kyslot [Synthesis and physical-chemical properties of 2-((4-R-3-(morpholinomethylen)-4H-1,2,4-triazole-5yl)thio)acetic acid]. Current issues in pharmacy and medicine: science and practice, (3), 18-21. [in Ukrainian].
Ignatova, T. V., Kaplaushenko, A. G., & Frolova, Yu. S. (2019). Stvorennia, doslidzhennia fizychnykh i khimichnykh vlastyvostei 2-((4-R-5-fenetyl-4H-1,2,4-triazol-3-il)tio)etanovykh(propanovykh, benzoinykh) kyslot i solei 2-((4-R-5-fenetyl-4H-1,2,4-triazol-3-il) tio)etanovykh kyslot [Creation, study of physical and chemical properties of 2-((4-R-5-phenethyl-4H-1,2,4-triazole-3-yl)thio)ethanоic(propanоic, benzoic)acids and salts of 2-((4-R-5-phenethyl-4H-1,2,4-triazole-3-yl)thio)ethanoic acid]. Current issues in pharmacy and medicine: science and practice, 12(2), 123-128. [in Ukrainian]. https://doi.org/10.14739/2409-2932.2019.2.170973
Samelyuk, Yu. G., Kaplaushenko, A. G., & Pruglo, E. S. (2014). Syntez ta aktoprotektorna aktyvnist solei 2-(5-(4-metoksyfenil-(3,4,5-trymetoksyfenil)-)-1,2,4-triazol-3-iltio)- atsetatnykh kyslot [Synthesis and actoprotective activity of salts 2-(5-(4-methoxyphenyl(3,4,5-trimethoxyphenyl))-1,2,4-triazole-3-ylthio)acetate acids]. Zaporozhye medical journal, (2), 107-111. [in Ukrainian].
Kaplaushenko, A. G. (2013). Vyvchennia farmakokinetyky morfolinii 2-(5-(4-pirydyl)-4-(2-metoksyfenil)-1,2,4-tryazol-3-iltio)atsetatu [The study of pharmacokinetics of morpholinium 2-(5-(4-pyridyl)-4-(2-methoxyphenyl)-1,2,4-triazol-3-ylthio)acetate]. Farmatsevtychnyi zhurnal, (6), 88-92. [in Ukrainian].
Aksyonova, I. I., Pruglo, Ye. S., Panasenko, O. I., & Knysh, Ye. H. (2015). Aktoprotektorna aktyvnist solei 2-((4-amino-5-R1-4N-1,2,4-triazol-3-il)tio)otstovykh kyslot [Actoprotective activity of the salts 2-((4-amino-5-R1-4Н-1,2,4-triazole-3-yl)thio)acetic acids]. Odeskyi medychnyi zhurnal, (3), 16-19. [in Ukrainian].
Samelyuk, Y. G., Kaplaushenko, A. G. (2013). Syntez ta fizyko-khimichni doslidzhennia hidrazydiv ta ilidenhidrazydiv 2-(5-(4-metoksyfenil), (3,4,5-trymetoksyfenil)-1,2,4-tryazol- 3-iltio) atsetatnykh kyslot [The synthesis and physical-chemical research of hydrazides and ylidenhydrazides of 2-(5-(4-methoxyphenyl), (3,4,5-threemethoxyphenyl)-1,2,4-triazole-3-ilthio) acetate acids]. Farmatsevtychnyi zhurnal, (4), 66-71. [in Ukrainian].
Samelyuk, Yu. G., & Kaplaushenko, A. G. (2015). The synthesis and physicochemical properties of 2-(5-methoxyphenyl-1H-1,2,4-triazole-3-ylthio) acetonitriles and their iminoethers. Journal of Organic and Pharmaceutical Chemistry, 13(3), 57-62. https://doi.org/10.24959/ophcj.15.841
Sameluk, Yu. G., Belenichev, I. F., Abramov, A. V., Bukhtiyarova, N. V., Morguntsova, S. A., Pavlov, S. V., & Kaplaushenko, A. G. (2015). Doslidzhennia neiroprotektornoi aktyvnosti propil 2-(5-(3,4,5-trymetoksyfenil)-1H-1,2,4-triazol-3-iltio) atsetimidatu hidrokhlorydu [Study of neuroprotective activity of propyl 2-(5-(3,4,5- trimethoxyphenyl)-1H-1,2,4-triazole-3-ylthio)acetimidate hydrochloride]. Farmakolohiia ta likarska toksykolohiia, (6), 34-40. [in Ukrainian].
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