Objective: The purpose of this work is to synthesize new series of 4-((5-((cyclohexylmethyl)thio)-4-R1-4H-1,2,4-triazol-3-yl)methyl)morpholines and 4-((4-R1-5-(pyridin-2-ylthio)-4H-1,2,4-triazol-3yl)methyl)morpholines using a microwave synthesis system. Material and Method: As starting compounds are used 4-R1-3-(morpholinomethyl)-4H-1,2,4-triazole-5thioles (where, R1=H, methyl, ethyl, phenyl, amino). Synthesis was carried out using a microwave synthesis system Milestone Flexi Wave. The structure of synthesized compounds is confirmed by the use of modern methods of analysis 1 H NMR, 13 C NMR spectroscopy, elemental analysis and gas chromatography-mass spectrometry (GS/MS). Result and Discussion: As a result of the conducted experiment, the synthesis method is optimized for 4-((5-((cyclohexylmethyl)thio)-4-R1-4H-1,2,4-triazol-3-yl)methyl)morpholines and 4-((4-R1-5-(pyridin-2-ylthio)-4H-1,2,4-triazol-3-yl)methyl)morpholines by microwave irradiation. It was established that the reactions proceed to the end in all described conditions, but the reaction with the parameters t=10 min, T=160 о С is the most technologically optimal. This approach has allowed reducing energy costs and increasing the yield of target compounds. As a result, a class of new derivatives of 1,2,4-triazole has been obtained, which can be used in further pharmacological studies as valuable biological agents.
Objective:The aim of this work is the synthesis and studying of antimicrobial and antifungal properties of the ylidenhydrazides of 2- ((4-R-5-R1-4H-1,2,4-triazol-3-yl)thio)acetaldehydes with the establishment of structure-activity relationships of the synthesized compounds.Material and Method: Determination of antimicrobial and antifungal activity was performed by discdiffusion method (DDM) on series of gram positive and gram negative bacteria such as Corynebacterium pseudodiphtheriticum, Pseudomonas aeruginosa, Enterococcus faecalis, Proteus vulgaris, Escherichia coli, Salmonella spp., Staphylococcus saprophyticus, Staphylococcus aureus, Streptococcus pyogenes, Candida.Result and Discussion: A new series of ylidenhydrazides of 2-((4-R-5-R1-4H-1,2,4-triazol-3yl)thio)acetaldehydes were synthesized and their structures were confirmed by modern methods of instrumental analysis: IR and 1 H-spectroscopy, elemental analysis and GS\MS method. For 13 compounds, the antimicrobial and antifungal activities were studied on 10 strains of microorganisms in 3 different concentrations (0.1; 0.2; 0.5%). According to the results of the study, some regularities of the structureactivity relationship have been established. The obtained results can serve as a basis for the targeted search compounds with pronounced antibacterial action. An increasing the concentration of tested compounds predictably lead to increase on antimicrobial activity in almost all cases. The most active compound in our study is N'-(2-((5-methyl-4H-1,2,4-triazol-3-yl)thio)ethylidene)-4-nitrobenzohydrazide 3i (ZOI for Sta.s. and Sp in 0.5% concentration is 25 and 26 mm, respectively).
Objective: The purpose of this work is to study the hepatoprotective properties of potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazole-3-yl)thio)acetate on tetracycline and infectious hepatitis models in chickens. Material and Method: Biochemical examination of blood and liver serum was carried out on intact broiler chickens Cross Cobb 500. All groups of chickens were kept separately in different cages in the same room with the same microclimate parameters in accordance with the established requirements. Result and Discussion: Hepatoprotective effect of potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazole-3-yl)thio)acetate was established as a result of research on the model of hepatitis in chickens caused by tetracycline, which was not lower than the referent drug-Thiotriazolin ®. The biochemical study results demonstrated hepatoprotective properties of the combination of the above compound with the antibiotic Saroflox ® , combination of potassium 2-((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazole-3-yl) thio) acetate with classical antibiotic Enrofloxacin ® on the model of infectious hepatitis.
Objective: The aim of the research is the histological study of the corrective effect of the compound potassium 2((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3yl)thio)acetate (PKR-173) with different antibiotics on the state of chicken's liver under infection by Pseudomonas aeruginosa. Material and Method: The histological study was carried out on the levers of intact chickens (intact control); chickens that were infected by the strain of Pseudomonas aeruginosa (controlled pathology); chickens that had (before being infected by Pseudomonas aeruginosa
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.