Derivatives of 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines as increasing efficiency substances
In today's society, especially in eastern countries such as China, Japan etc., the problem of fatigue and even death at work is acute. One of the solution to this problem is complex therapy with increasing efficiency drugs. Derivatives of 1,2,4-triazole have already proven themselves as potential compounds for pharmacological correction of fatigue. Compounds were synthesized at the Department of toxicological and inorganic chemistry ZSMU. Using method of forced swimming on a group of white nonlinear rats activity of anti-fatigue of the compounds were analyzed. Having analyzed the data of pharmacological correction of fatigue for 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines, it should be noted that this series of compound do not show anti-fatigue effect. Introduction in molecule 3- (nonylthio)-5-(thiophen-2-ylmethyl)-4H- 1, 2, 4-triazol-4-amine 4-fluorbenzylidene, 4-(dimethylamino) benzylidene, 4- methoxybenzylidene, 2-chloro-6-fluorobenzylidene radicals lead to increase actoprotective effect. The most active compound is N-(2-chloro-6-fluorobenzylidene)-3-(nonylthio)-5-(thiophen- 2- ylmethyl)- 4H- 1, 2, 4- triazol- 4-amine which exceeds the standard (riboxin).
Aksonova I. I., Shcherbyna R. O., Panasenko O. I. et. al. Ukrainskyi biofarmatsevtychnyi zhurnal. 2014.; 6: 78–82.
Cervantes-Elizarrarás, A., Piloni-Martini, J., Ramírez-Moreno, E., Alanís-García, E., Güemes-Vera, N., Gómez-Aldapa, C. A., del Socorro Cruz-Cansino, N. Ultrasonics Sonochemistry. 2017; Vol. 34: 371–379.
Chen, W., Su, H., Xu, Y., Jin, C. Scientific Reports. 2017.; 7:405–414.
Rodionova N., Manukovskaya M., Kolomnikova Ya. et. al. Vestnik Voronezhskogo gosudarstvennogo universiteta inzhenernyih tehnologiy. 2015.; Vol. 66, Iss. 4: 98–103.
Danilchenko D. M., Parchenko V. V., Panasenko O. I., Knysh Ye. H. Aktualni pytannia farmatsevtychnoi i medychnoi nauky ta praktyky. 2015.; 3: 93–97.
Kumar, G. S., Prasad, Y. R., & Chandrashekar, S. M. (2013). Synthesis and pharmacological evaluation of novel 4-isopropylthiazole-4-phenyl-1, 2, 4-triazole derivatives as potential antimicrobial and antitubercular agents. Medicinal Chemistry Research, 22(2), 938-948.
Methodological recommendations for the removal of laboratory animals from the experiment. 1986; 12 p.
Parchenko V. V. Farmatsevtychnyi zhurnal. 2012.; 3: 43–48.
Patel, N. B., Khan, I. H., Pannecouque, C., & De Clercq, E. (2013). Anti-HIV, antimycobacterial and antimicrobial studies of newly synthesized 1, 2, 4-triazole clubbed benzothiazoles. Medicinal Chemistry Research, 22(3), 1320-1329.
Pattan, S., Gadhave, P., Tambe, V., Dengale, S., Thakur, D., Hiremath, S. V., & Deotarse, P. (2012). Synthesis and evaluation of some novel 1, 2, 4-triazole derivatives for antmicrobial, antitubercular and anti-inflammatory activities. Indian Journal of Chemistry Section B 51(1):297-301.
Preclinical research of medicinal products: Methodical recommendations / Ed. Corresponding Member AMS of Ukraine O. V. Stefanova. 2001; 528 p.
Safonov A. A. (2016) Synthesis and physicochemical properties of 3-(alkylthio)-5-thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amines derivatives // Ukrainian biopharmaceutical journal. 3-4(43):50-54.
Shcherbyna R.O. Farmatsevtychnyi chasopys. 2014.; 4: 145–150.
Thakkar, S. S., Thakor, P., Doshi, H., & Ray, A. (2017). 1,2,4-triazole and 1,3,4-oxadiazole analogues: synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities. Bioorganic & Medicinal Chemistry. 25(15):4064-4075. doi: 10.1016/j.bmc.
Tkachenko, A., Zazharsky, V., Bilan, M., & Kovaleva, L. (2010). Some peculiarities of bovis tuberculosis display in long not favourably farm. News of Dniproptrovsk State Agrarian and Economic University, (1), 100-103
Varynskyi, B., Knysh, Y., Parchenko, V., Panasenko, O., & Kaplaushenko, A. (2015). The study of retention regularities for the potential drug substances of 1,2,4-triazol-3-ylthioacetic acids and their salts series by the method of HPLC/DAD-MS. Journal Of Organic And Pharmaceutical Chemistry, 13(4), 68-75.
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