Derivatives Of Pyrimidine Bases Research Articles

The effect of liposomal composition with encapsulated potassium orotate on the macrophage link of immunity in the treatment of wounds

In veterinary medicine, treatment of wounds is one of the most important areas. A possible way to solve the problem of wound treatment is to activate the body's own protective reserves, primarily the immune system. Various immunostimulants and immunomodulators are widely used to activate the immune system. Known immunostimulants are derivatives of pyrimidine bases, in particular, potassium orotate (potassium salt of orotic acid). Orotic acid is found in milk and colostrum of animals. The use of orotic acid or its salts as immunostimulants is difficult due to their low bioavailability determined by their solubility in water. It is possible to increase the effectiveness of immunostimulators based on potassium orotate by including it in liposomes. Liposomes with encapsulated potassium orotate were obtained by shaking. The aim of the research was to study the activation of immunity macrophage link by liposomes with encapsulated potassium orotate. Evaluation of the effectiveness of the liposomal drug was carried out on rat wound models and on post-castration wounds of suckling pigs. Animal experiments were conducted according to bioethical norms. Complete wound healing in rats with the use of liposomal gel occurred on day 2, earlier than in the control with the use of Monclavit-1, while in the experimental group, compared with the control group, the content of leukocytes, lymphocytes, monocytes, platelets and granulocytes was significantly higher. The healing of surgical wounds in piglets after castration with the use of liposomal gel occurred 2 days earlier than with the use of the drug "Monclavit-1". There were no complications in both groups. Based on the analysis of literature data and the results of our own research, a scheme of the mechanism of action of a liposomal drug was proposed. The hypothesis about the mechanism of influence of liposomal composition on the macrophage link of immunity has been presented.

The Effect of Whole Blood and Bone Marrow with the Addition of Pyrimidine-2,4(1h,3h)-dione Thietanyl Derivatives on Free Radical Oxidation.

It is relevant to study the general patterns and identify non-specific mechanisms of body protective and adaptive reactions violation, which can lead to the various pathological processes and develop principles for the correction of these disorders. One of the therapy and prevention directions is the search for new medicines. In recent years, new derivatives of pyrimidine bases have been synthesized and studied. Pyrimidine-based medicines have a membrane-stabilizing and immunomodulatory effect and can normalize metabolic disorders and increase the oxidative activity of leukocytes. Disruption of the free radical oxidation processes, the generation of reactive oxygen species and lipid peroxidation, including in whole blood and bone marrow, has gained importance in recent years. Each reaction was monitored by thin layer chromatography. 1H, 13C, and 15N NMR spectra were recorded (chemical shifts were expressed as δ-values). We studied the effect of 6-methyl-3-(thietan- 3-yl)pyrimidine-2,4(1H,3H)-dione on the generation of reactive oxygen species (ROS) in the whole blood and bone marrow using the study of whole blood spontaneous and stimulated chemiluminescence (CL). CL methods make it possible to quickly and easily assess the studied material (whole blood, bone marrow) effect on free radical oxidation. Using CL methods, it is possible to reveal the presence of medicines' pro- or antioxidant properties, opening up new possibilities in the search for substances with antioxidant properties and comparing their activity. Alkylation of 6-methylpyrimidine-2,4(1H,3H)-dione by 2-chloromethylthiirane in protic solvents in the presence of alkali leads to the formation of an N-thietane derivative. NMR spectroscopy showed that 6-methylpyrimidine-2,4(1H,3H)-dione was alkylated at position 3. The oxidation reactions of N-(thietan-3-yl)pyrimidine-2,4(1H,3H)-dione were studied, and it was determined that, depending on the excess of the oxidizing agent and the duration of the process, N-(1-oxothietan-3-yl)- or N-(1,1-- dioxothietan-3-yl)pyrimidine-2,4(1H,3H)-diones were formed. The effects of free radical oxidation processes of new biologically active pyrimidine-2,4(1H,3H)-diones were studied. New pyrimidine-2,4(1H,3H)-diones increase the general adaptive capabilities of the body and have protective effects in extreme conditions.

Synthesis of cyano derivatives of pyrimidine bases and their effect on blood leukocyte system

Synthesis of cyano derivatives of pyrimidine bases and their effect on blood leukocyte system

Polymethylene derivatives of pyrimidine nucleic bases bearing ω-functional groups

N1-Acyclic derivatives of pyrimidine bases (uracil, thymine, and cytosine) with hydrophobic polymethylene chains containing various functional groups in an ω-position of the alkyl substituent were synthesized. Their physicochemical properties and inhibitory effect on the HIV reverse transcriptase and human DNA topoisomerase I were studied.

Proton NMR studies on the interaction of alkyl derivatives of pyrimidine bases, their nucleosides and nucleotides with bovine serum albumin

Proton NMR studies on the interaction of alkyl derivatives of pyrimidine bases, their nucleosides and nucleotides with bovine serum albumin

Oxidation of 1,3-dimethyl derivatives of pyrimidine bases with m-chloroperbenzoic acid.

Oxidation of 1, 3-dimethylthymine (1), 1, 3-dimethyluracil (2), and 5-fluoro-1, 3-dimethyluracil (3) with m-chloroperbenzoic acid were investigated. 1 gave the cis diol 5, 6-dihydrothymine derivative (4) stereoselectively. Its stereostructure was definitely determined by an X-ray analysis. 2 afforded 7, 8, and 9, and 3 afforded 8.

Nonglycoside analogs of the nucleotides 12. Photoionization mass spectra of the hydroxy-alkyl derivatives of pyrimidine bases of nucleic acids

1. Study has been made of the energy relations for the principal modes of molecular ion breakdown in the compounds under study here. 2. The upper filled molecular orbital in these compounds is occupied by theπ electrons of the pyrimidine ring. 3. Formation of [B+2H]+ ions is inhibited by introducing a methyl substituent in the pyrimidine ring and by lengthening the hydroxyalkyl chain.