The results of determining the indicators of the morphological composition of the blood of animals and individual biochemical indicators using a potential drug with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bro

M. V. Ohloblina, I. V. Bushuieva, V. Parchenko
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At this stage of research, it is known that such 1,2,4-triazole derivatives as 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol have a wide spectrum of biological activity. Interest for further thorough research is precisely the antimicrobial and antifungal effects. The introduction into medical and veterinary practice of newly created drugs for the treatment of fungal diseases on the skin of animals requires further studies of the properties of these compounds and their mixtures.\nThe aim of the work was to determine the indicators of the morphological composition of the blood of animals and individual biochemical indicators when using a preparation with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol in thistle seed oil.\nMaterials and methods. The material for laboratory research was serum and blood plasma, stabilized by adding trilon-B, tissue biopsy. Indicators were determined in healthy animals and experimentally diseased animals on the third and tenth days after the onset of the disease according to the generally accepted method. During the research, in the course of treatment, general clinical examinations and local examinations of purulent wounds were carried out, as well as blood samples taken from each head of the sheep in the experimental and control groups before the beginning and on the third and tenth days of the experiment. The purulent-inflammatory process was caused by injuring the soft tissues in the groin area on the left side, with the help of a specially made template, followed by dilation of the muscle tissue with an angiotrip and implantation of aerobic-anaerobic surgical infection cultures taken from the bed. The resulting wounds had the following dimensions: 10 cm in length, 1 cm in width, and 2 cm in depth. As early as 24 hours after induction of experimental purulent inflammation, characteristic clinical signs appeared in sheep. The general condition of all 12 animals was somewhat depressed, the appetite was normal. The body temperature was in the range of 38.6–40.3 °C, the pulse was 76–82 beats, and the frequency of respiratory movements was 16–18 per minute. The frequency of scar contractions was 3–6 times in 2 minutes. During the examination, slight swelling was also found in the area of the wound and its edges. There was a small amount of serous-bloody exudate on the surface of the wound. On the 3rd day, the maximum manifestation of clinical signs of acute purulent inflammation was observed in all 12 sheep. In particular, the general condition of the animals is depressed. A partial loss of appetite was observed. General temperature 40.4–40.8 °C, pulse 75–82 beats, frequency of respiratory movements 18–22 per minute. The frequency of scar contractions was 3–6 times in 2 minutes. Visible mucous membranes are pale pink in color. When pressing on the area of the wound, a serous-purulent exudate was observed.\nResults. Laboratory indicators of blood and tissue biopsy that are more optimal than in the control group confirm positive changes in the clinical status of the animals in the experimental group. The use of a potential preparation with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol in thistle seed oil leads to faster healing of purulent wounds, in relation to the use of “Vetmikoderm” liniment (control group). The difference in the areas of the wound defect on the 10–11th day was 17.5 %. Clinical studies were confirmed by laboratory studies and wound biopsies.\nConclusions. The preparation with two compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol had pronounced pharmacokinetic parameters and was bioavailable.\n ","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"63 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current issues in pharmacy and medicine: science and practice","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.14739/2409-2932.2022.3.263015","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

The introduction of new domestic highly effective and safe medicines into medical and veterinary practice is an important task of modern pharmaceutical science. Continuation of the search and conduct of research to bring the biological activity of 1,2,4-triazole derivatives is one of the promising areas of such activity. At this stage of research, it is known that such 1,2,4-triazole derivatives as 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol have a wide spectrum of biological activity. Interest for further thorough research is precisely the antimicrobial and antifungal effects. The introduction into medical and veterinary practice of newly created drugs for the treatment of fungal diseases on the skin of animals requires further studies of the properties of these compounds and their mixtures. The aim of the work was to determine the indicators of the morphological composition of the blood of animals and individual biochemical indicators when using a preparation with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol in thistle seed oil. Materials and methods. The material for laboratory research was serum and blood plasma, stabilized by adding trilon-B, tissue biopsy. Indicators were determined in healthy animals and experimentally diseased animals on the third and tenth days after the onset of the disease according to the generally accepted method. During the research, in the course of treatment, general clinical examinations and local examinations of purulent wounds were carried out, as well as blood samples taken from each head of the sheep in the experimental and control groups before the beginning and on the third and tenth days of the experiment. The purulent-inflammatory process was caused by injuring the soft tissues in the groin area on the left side, with the help of a specially made template, followed by dilation of the muscle tissue with an angiotrip and implantation of aerobic-anaerobic surgical infection cultures taken from the bed. The resulting wounds had the following dimensions: 10 cm in length, 1 cm in width, and 2 cm in depth. As early as 24 hours after induction of experimental purulent inflammation, characteristic clinical signs appeared in sheep. The general condition of all 12 animals was somewhat depressed, the appetite was normal. The body temperature was in the range of 38.6–40.3 °C, the pulse was 76–82 beats, and the frequency of respiratory movements was 16–18 per minute. The frequency of scar contractions was 3–6 times in 2 minutes. During the examination, slight swelling was also found in the area of the wound and its edges. There was a small amount of serous-bloody exudate on the surface of the wound. On the 3rd day, the maximum manifestation of clinical signs of acute purulent inflammation was observed in all 12 sheep. In particular, the general condition of the animals is depressed. A partial loss of appetite was observed. General temperature 40.4–40.8 °C, pulse 75–82 beats, frequency of respiratory movements 18–22 per minute. The frequency of scar contractions was 3–6 times in 2 minutes. Visible mucous membranes are pale pink in color. When pressing on the area of the wound, a serous-purulent exudate was observed. Results. Laboratory indicators of blood and tissue biopsy that are more optimal than in the control group confirm positive changes in the clinical status of the animals in the experimental group. The use of a potential preparation with a mixture of two active compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol in thistle seed oil leads to faster healing of purulent wounds, in relation to the use of “Vetmikoderm” liniment (control group). The difference in the areas of the wound defect on the 10–11th day was 17.5 %. Clinical studies were confirmed by laboratory studies and wound biopsies. Conclusions. The preparation with two compounds: 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine and 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol had pronounced pharmacokinetic parameters and was bioavailable.  
用两种活性化合物:4-((5-(癸基硫)-4-甲基- 4h -1,2,4-三唑-3-基)甲基)啉和5-(2-氟苯基)-4-(4-苯基)混合的潜在药物测定动物血液形态组成指标和个体生化指标的结果
将高效安全的国产新药引入医学和兽医实践是现代药学的一项重要任务。继续寻找和开展研究使1,2,4-三唑衍生物具有生物活性是这类活性的有前景的领域之一。在此研究阶段,已知4-((5-(癸基硫)-4-甲基- 4h -1,2,4-三唑-3-基)甲基)啉和5-(2-氟苯基)-4-((4-溴苯基)基)氨基-1,2,4-三唑-3-硫醇等1,2,4-三唑衍生物具有广谱的生物活性。进一步深入研究的兴趣正是抗菌和抗真菌作用。将用于治疗动物皮肤真菌疾病的新发明药物引入医学和兽医实践,需要进一步研究这些化合物及其混合物的特性。本研究的目的是测定两种活性化合物(4-(5-(癸硫)-4-甲基- 4h -1,2,4-三唑-3-基)甲基)啉和5-(2-氟苯基)-4-((4-溴苯基)基)氨基-1,2,4-三唑-3-硫醇)混合制剂中动物血液形态组成指标和个体生化指标。材料和方法。实验室研究的材料为血清和血浆,加入万亿b稳定,组织活检。在发病后第3天和第10天,按普遍接受的方法测定健康动物和实验患病动物的各项指标。研究过程中,在治疗过程中进行一般临床检查和化脓性伤口局部检查,并在实验开始前、实验第3天和第10天分别对实验组和对照组羊的每头羊采集血液样本。脓性炎症过程是在特制模板的帮助下,损伤左侧腹股沟区域的软组织,然后用血管穿刺扩张肌肉组织,并植入从床上取出的好氧-厌氧手术感染培养物。由此产生的伤口尺寸如下:长10厘米,宽1厘米,深2厘米。早在实验性化脓性炎症诱导后24小时,绵羊就出现了特征性的临床体征。12只动物总体情况稍显抑郁,食欲正常。体温38.6 ~ 40.3℃,脉搏76 ~ 82次,呼吸运动频率16 ~ 18次/ min。瘢痕收缩频率为2分钟3 ~ 6次。检查时,伤口及其边缘也有轻微肿胀。伤口表面有少量浆血渗出物。试验第3天,12只羊均出现急性化脓性炎症的临床症状。特别是,动物的总体状况是沮丧的。观察到部分食欲不振。全身体温40.4 ~ 40.8℃,脉搏75 ~ 82次,呼吸频率每分钟18 ~ 22次。瘢痕收缩频率为2分钟3 ~ 6次。可见粘膜呈淡粉色。按压创面时,可见浆液-化脓性渗出物。血液和组织活检的实验室指标均优于对照组,证实了实验组动物临床状况的积极变化。与使用“Vetmikoderm”搽剂(对照组)相比,使用含有两种活性化合物的潜在制剂:4-((5-(癸硫)-4-甲基- 4h -1,2,4-三唑-3-基)甲基)morpholine和5-(2-氟苯基)-4-((4-溴苯基)基)氨基-1,2,4-三唑-3-硫醇在蓟籽油中的混合物,可以更快地愈合化脓性伤口。10 ~ 11天创面缺损面积差异为17.5%。临床研究得到了实验室检查和伤口活检的证实。4-((5-(癸基硫)-4-甲基- 4h -1,2,4-三唑-3-基)甲基)啉和5-(2-氟苯基)-4-((4-溴苯基)基)氨基-1,2,4-三唑-3-硫醇具有明显的药动学参数和生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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