Browsing by Author "Shcherbyna, Roman"

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    An investıgation of the pharmacokinetics and potential metabolites of potassium 2-((4-amino-5- (morfolinometyl)-4h-1,2,4-triazol-3-yl)thıo) acetate on rats
    (Ankara Üniversitesi, 2020-05-31) Shcherbyna, Roman; Eczacılık Fakültesi
    Objective: The purpose of this work is to study the designated pharmacokinetic parameters and possible metabolites of the substance potassium 2-((4-amino-5-(morfolinometyl)-4H-1,2,4-triazol-3-yl)thio)acetate by intragastric introduction to rats. Material and Method: The study was performed on Wistar rats. The following parameters were calculated to evaluate the pharmacokinetic properties: area under the pharmacokinetic curve (AUC), apparent clearance (CL), elimination rate constant (K), volume of distribution (VT), serum half-life (t1⁄2). Separation was performed using Agilent 1260 Infinity HPLC system. Result and Discussion: The determination of the concentration of potassium 2-((4-amino-5-(morfolinometyl)-4H-1,2,4-triazol-3-yl)thio)acetate in serum was performed for 0.08 (5 min), 0.25 (15 min), 0.75 (45 min), 2.5, 7.5, 13.5 and 24 hours. It was found that in the serum of rats the maximum concentration of the injected substance was reached almost immediately after administration, namely for 5 min with an average value at the level of 279,67 µg/ml. Thereafter, the concentration decreases mono-exponential, which indicates that the distribution and elimination occur at the same rate. The area under the pharmacokinetic curve is AUC = 150,8998 µg*h/ml. The serum half-life of the specified substance is established (t1⁄2 = 0.32 hours). Based on the obtained chromatograms and mass spectra, 5 possible metabolites of potassium 2-((4-amino-5-(morfolinometyl)-4H-1,2,4-triazol-3-yl)thio)acetate (PKR-173)were determined by intragastric introduction to rats. Amaç: Bu çalışmanın amacı, sıçanlara intragastrik olarak uygulanan potasyum 2-((4-amino-5-(morfolinometil)-4H-1,2,4-triazol-3-il)tiyo) asetat maddesinin, belirli farmakokinetik parametrelerini ve olası metabolitlerini incelemektir. Gereç ve Yöntem: Çalışma Wistar sıçanları üzerinde gerçekleştirilmiştir ve farmakokinetik özellikleri değerlendirmek için aşağıdaki parametreler hesaplanmıştır: Farmakokinetik eğri altındaki alan (AUC), toplam klerens (CL), eliminasyon sabiti (K), toplam dağılım hacmi (VT) ve serum yarılanma ömrü (t1/2). Ayırım, Agilent 1260 Infinity HPLC sistemi kullanılarak gerçekleştirilmiştir. Sonuç ve Tartışma: Kan serumundaki potasyum 2-((4-amino-5-(morfolinometil)-4H-1,2,4-triazol-3-il)tiyo) asetat konsantrasyonunun belirlenmesi, 0.08 (5 dakika), 0.25 (15 dakika), 0.75 (45 dakika), 2.5, 7.5, 13.5 ve 24 saat boyunca gerçekleştirilmiştir. Sıçanların kan serumunda, enjekte edilen maddenin maksimum konsantrasyonuna, uygulamadan hemen sonra, ortalama 279.67 μg/ml'lik bir değerle ve 5 dakika içinde ulaşıldığı bulunmuştur. Bu aşamadan sonra, konsantrasyon mono-exponential olarak azalmıştır ve bu durum dağılım ve eliminasyonun aynı oranda devam ettiğini göstermiştir. Farmakokinetik eğri altındaki alan (AUC) = 150.8998 μg*h/ml olup, belirtilen maddenin serum yarılanma ömrü belirlenmiştir (t1/2 = 0,32 saat). Elde edilen kromatogramlara ve kütle spektrumlarına dayanarak, sıçanlara intragastrik uygulama sonucunda, 5 adet olası potasyum 2-((4-amino-5-(morfolinometil)-4H-1,2,4-triazol-3-il)tiyo) asetat metaboliti belirlenmiştir.
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    Histological study of a corrective influence of a compound potassium 2-((4-amino-5-(morpholinomethyl)- 4h-1,2,4-triazol-3-yl)thio)acetate (pkr-173) on the state of chicken's liver under infection by pseudomonas aeruginosa
    (Ankara Üniversitesi, 2020) Vashchyk, Yevgenia; Shcherbyna, Roman; Parchenko, Volodymyr; Bushueva, Inna; Gutyj, Bogdan; Fotina, Hanna; Fotina, Tatiana; Stronskyi, Yuriy; Eczacılık Fakültesi
    otassium 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) preventive input of the compound PKR-173 with the classic antibiotic Enrofloxacin or with Saroflox (undergoing research); or were input Thiotriazolin with the classic antibiotic Enrofloxacin. Result and Discussion: As a result, it is stated, that preventive input of the compound PKR-173 with reseachable antibiotic Saroflox, as well as with classic antibiotic Enrofloxacin and Thiotriazolin with antibiotic Enrofloxacin, to chickens infected with pseudomonas aeruginosa, prevents from chickens' livers developing stereotypical morphological changes characteristic of nonspecific reactive hepatitis. Analysis of quantitative characteristics of pathological process that developed in chicken's liver infected with pseudomonas aeruginosa, and the corrective influence of researched methods showed that the compound PKR-173 with antibiotic Saroflox believably lowers displays of all signs of pathology compared to the controlled pathology
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    Microwave-assisted synthesis of some new derivatives of 4-Substıtuted-3-(Morpholınomethyl)-4H-1,2,4- Triazole-5-Thioles
    (Ankara : Ankara Üniversitesi, 2019) Shcherbyna, Roman; https://orcid.org/0000-0002-9742-0284; Eczacılık Fakültesi
    Objective: The purpose of this work is to synthesize new series of 4-((5-((cyclohexylmethyl)thio)-4-R1-4H1,2,4-triazol-3-yl)methyl)morpholines and 4-((4-R1-5-(pyridin-2-ylthio)-4H-1,2,4-triazol-3- yl)methyl)morpholines using a microwave synthesis system. Material and Method: As starting compounds are used 4-R1-3-(morpholinomethyl)-4H-1,2,4-triazole-5- thioles (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 1H NMR, 13C 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 оС 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.
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    SYNTHESIS, ANTIMICROBIAL AND ANTIFUNGAL ACTIVITY OF YLIDENHYDRAZIDES OF 2-((4-R-5-R1-4H-1,2,4-TRIAZOL-3-YL)THIO)ACETALDEHYDES
    (Ankara Üniversitesi, 2021) Shcherbyna, Roman; Other; Other
    Amaç: Bu çalışmanın amacı, 2-(4-R-5-R1-4H-1,2,4-triazol-3-yl)tio)asetaldehitlerin bir dizi ilidenhidrazidinin sentezi ve antimikrobiyal ve antifungal özelliklerinin yapı-etki ilişkisi kurularak incelenmesidir. Gereç ve Yöntem: Antimikrobiyal ve antifungal aktivitenin tespiti, aşağıdaki mikroorganizma türleri için disk-difüzyon yöntemi ile gerçekleştirilmiştir: Corynebacterium pseudodiphtheriticum, Pseudomonas aeruginosa, Enterococcus faecalis, Proteus vulgaris, Escherichia coli, Salmonella spp., Staphylococcus saprophyticus, Staphylococcus aureus, Streptococcus pyogenes, Candida. Sonuç ve Tartışma: Yeni 2-((4-R-5-R1-4H-1,2,4-triazol-3-yl)tio)asetaldehitlerin ilidenhidrazidleri sentezlenmiştir. Yapıları modern analiz yöntemleri olan IR, 1H spektroskopisi, element analizi ve GS\MS yöntemi ile doğrulanmıştır. Sentezlenen 13 bileşik için antimikrobiyal aktivite, 3 farklı konsantrasyonda (0.1; 0.2; % 0.5) 10 mikroorganizma suşu üzerinde çalışılmıştır. Çalışmanın sonuçlarına göre, bazı yapı-etki ilişkileri kurulmuştur. Elde edilen sonuçlar, belirgin antibakteriyel etkiye sahip bileşikler için hedeflenen araştırmanın temelini oluşturabilir. Test maddelerinin konsantrasyonunun artırılmasının, neredeyse tüm durumlarda antimikrobiyal etkiyi artıracağı tahmin edilmektedir. Çalışmamızdaki en aktif bileşik N'-(2-((5-metil-4H-1,2,4-triazol-3-il)tiyo)etiliden)-4-nitrobenzohidrazid 3i’dir (ZOI Sta.s. ve Sp. - 25 ve 26 mm % 0,5 konsantrasyonda).
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    The research of 1,2,4-triazole derivatives hepatoprotective activity under tetracycline and infectious hepatitis
    (Ankara : Ankara Üniversitesi, 2019) Shcherbyna, Roman; Vashchyk, Yevgenia; https://orcid.org/0000-0002-9742-0284; Eczacılık Fakültesi
    Objective: The purpose of this work is to study the hepatoprotective properties of potassium 2-((4-amino5-(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)-4H1,2,4-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.