Effects Of Pyrimidine Derivatives Research Articles

Diverse Pharmacological Potential of Various Substituted Pyrimidine Derivatives

Abstract: In many significant bioactive heterocyclic compounds, the six-membered ring pyrimidines play a major role as bioactive components. There is a lot of room for innovation in the fields of medicinal chemistry and the chemical industries because of the numerous pyrimidine synthesis methods and their varied reactions. The pharmacological effects of pyrimidine derivatives include anticonvulsant, antibacterial, antifungal, antiviral, antitubercular, anticancer, antimicrobial, antihypertensive, antiulcer, anti-inflammatory, antimalarial, antioxidant, analgesic, sedative, anti-depressive, antipyretic properties, etc. The synthetic adaptability of pyrimidine has made it possible to create a wide range of structurally different analogs, including analogs from substitution on the pyrimidine ring at various places, which has aided the design of a wide variety of therapeutic targets. This review's goal is to examine the pharmacological effects of numerous pyrimidine derivatives. This review provides an overview of pyrimidine compounds for biological activities and examines the novel pharmacological molecules containing pyrimidine rings in the future.

Моделирование оксидативного и психоэмоционального стресса у крыс с влиянием производных пиримидина

Моделирование оксидативного и психоэмоционального стресса у крыс с влиянием производных пиримидина

The study of the apoptogenic effect of pyrimidine derivatives on murine leukemia cells

BACKGROUND: In the light of the recent findings concerning the role of apoptosis and of tumor cell enzymes in cancer chemotherapy, the interest in pyrimidine derivatives has greatly increased. Thio- and hydrazine- pyrimidines were synthesized as potential antimetabolites inhibiting the biosynthesis of nucleic acids. Some of them demonstrated biological activity, including antibacterial and antitumor action. The aim of this study was to analyze the cytotoxic activity and the ability of some derivatives to induce apoptosis in murine leukemia cells. METHODS: Exponentially growing cells were incubated with compounds and after 24, 48, and 72 hours were stained with trypan blue and counted hemocytometrically. For detection of the cell fraction undergoing apoptosis, a morphological analysis was made using fluorescent dye propidium iodide. RESULTS: Eight thio- and hydrazine- pyrimidine derivatives were investigated. 2-Thiouracil and 6- hydrazinouracil did not influence the cell growth. 2,4-dithiouracil, 2-thio-4-hydrazinouracil, 2-hydrazinouracil, and 2-thio-5-fluorouracil decreased cell proliferation, but even at the highest studied concentration (1000 ?M) had no cytostatic action. Only high concentrations of 2,4-dihydrazinouracil and 2- chloro-4-hydrazinouracil showed a strong cytotoxic activity. The treatment with 2,4-dihydrazinouracil as well as with 5-fluorouracil caused the appearance of apoptotic cells with typical fragmented condensed nuclei, ghosts and apoptotic bodies. In contrast, dead cells treated with 2-chloro-4-hydrazinouracil did not show apoptotic morphology. CONCLUSION: Among studied eight thio- and hydrazine- pyrimidine derivatives only 2,4-dihydrazinouracil demonstrated strong apoptogenic activity. Its active concentrations were about 100 times higher than apoptogenic concentrations of 5-fluorouracil which points to different mechanisms of cytotoxic action.

Xymedon restores T-cell immune response inhibited by γ-irradiationin vivo: Interrelations with Ca2+-ATPase and DNA-relaxing activities

High radioprotective activity of xymedon was shown in mice. Radioprotective effects of this preparation were accompanied by restoration of the delayed-type hypersensitivity response and Ca2+-ATPase activity in splenocytes which were inhibited by γ-irradiation (3 Gy). At concentrations of 10−3 and 10−6 M xymedon stimulated the activity of DNA topoisomerase-I of splenocyte nuclei. Here we discuss a mechanism of radioprotective effects of pyrimidine derivatives associated with the inhibition of apoptosis of lymphoid cells and the stimulation of proliferation and differentiation of lymphoid precursor cells.

Effect of pyrimidine derivatives on adenylate cyclase system of immunocompetent cell regulationin vitro

The pyrimidine derivatives xymedone and diucifon decrease the activity of adenylate cyclase, as shown in experiments on thymocytes and lymphocytes of guinea pig lymph nodes and human peripheral blood lymphocytes. Inhibition of the enzyme depends on the subpopulation and species appurtenance of immunocompetent cells. The relationship between the results and effects of pyrimidine derivatives in experiment and clinical setting is discussed.

Effect of pyrimidine derivatives: Xymedone and diuciphone on bioenergetic processes of mitochondria

The stimulation of oxygen consumption in the presence of incubative medium just as excessive quantity of oxidation substrate, so oxidation phosphorylation disconnector of 2,4-dinitrophenol is shown on thymocytes of not pedigree he-rats obtaining xymedone (3 mg/kg and 30 mg/kg) and diuci phone (30 mg/kg) during 9 and 30 days. The effect of xymedone is dosedependent and more pronounced than the effect of diuciphone. The uniform effect of xymedone on mitochondrion respiration of thymocytes and isolated mitochondria of the liver is shown.

Effects of Pyrimidine Derivatives on RNA-Dependent RNA Polymerase of Mengovirus-Infected Fogh and Lund (FL) cells

Two newly synthesized pyrimidine derivatives were found to possess antiviral activity against Mengovirus in Fogh and Lund (FL) cells and in a cell-free system. The inhibitory effect on RNA-dependent RNA polymerase of Mengovirus-infected FL cells was assayed using 14C-UTP as precursor. Addition of 50 or 100 muM of the inhibitors in a cell-free system of crude enzyme and nucleoside triphosphate medium for 60 min incubation at 37 degrees C resulted in about 40 to 60% lower counting rates for drug-treated reaction mixtures. The analysis of the polymerase synthesis product (virus RNA extracted from the cell-free reaction mixture and deproteinized by the phenol-SDS method) was carried out by means of agarose-acrylamide gel electrophoresis. The main finding was a reduction of single-stranded Mengovirus RNA (RNase-sensitive and LiCl-precipitable). The rates of synthesis of the replicative intermediate (LiCl-precipitable) and the replicative form of RNA (LiCl-soluble) were not significantly influenced.