[(N-aryl)piperazinyl]butylpyrimidine derivatives with neurotropic and actoprotective properties was written by Andronati, S. A.;Soboleva, S. G.;Zamkovat, A. V.;Karasyova, T. L.;Rakipov, I. M.;Tsymbal, D. I.. And the article was included in Zhurnal Organichnoi ta Farmatsevtichnoi Khimii in 2016.Quality Control of 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one The following contents are mentioned in the article:
In this study the potential ligands of 5-HT1A receptors – arylpiperazines containing the residues of tetrahydropyrimidine as terminal fragments, compounds I·HCl [R1 = Pr-i, R2 = H, Me-2, Me-3, X = S; R1 = Pr-n, R2 = Me-3, X = O; R1 = Et, R2 = Me-2, X = S] and II·HCl, and dihydropyrimidine III·2HCl have been synthesized. The structures of I·HCl [R1 = Pr-i, R2 = H, Me-2, Me-3 X = S; R1 = Pr-n, R2 = Me-3 X = O;], II·HCl and III·2HCl have been confirmed by IR-spectroscopy, mass spectrometry and 1H-NMR-spectroscopy. Substances I [R1 = Pr-i, R2 = Me-2, Me-3, X = S; R1 = Pr-n, R2 = Me-3, X = O;] and III·2HCl inhibit the specific binding of the radioligand [3H]8-OH-DPAT with 5-HT1A receptors; it has been found that they have a pronounced affinity for these receptors. In the conflict situation test compounds of I·HCl [R1 = Pr-i, R2 = H, Me-2, Me-3, X = S; R1 = Pr-n, R2 = Me-3, X = O; R1 = Et, R2 = Me-2, X = S] and III·2HCl showed anxiolytic properties, whereas phenylpiperazinil- and o-tolylpiperazinilbutyl-4-methyl-5-isopropyl-1,2,3,-6-tetrahydropyrimidine-2-thio-6-ones (I·HCl; R1 = Pr-i, R2 = H, Me-2) exceeded the known drug buspirone by the level of the anxiolytic activity. The absence of this activity in compound II·HCl is probably due to the differences of substituents at N1 atom of the pyrimidine nucleus of compound II·HCl and other compounds of this series. It has been shown that on the model of hyperthermia all of these compounds in the dose range of 0.04-0.1 mg/kg possessed a high actoprotective activity increased the rat capacity work by 1.4-2.5 times compared to the control. The most active compound, I·HCl [R1 = Pr-i, R2 = Me-3, X = S;], in the ED50 dose of 0.04 mg/kg increased the duration of swimming in rats by 2.2 times (122%) compared to bemithylum. Some of the compounds (15 mg/kg) showed antihypoxic activity on the models of hemic [compounds I (R1 = Pr-i, R2 = Me-2, Me-3, S = S; R1 = Pr-n, R2 = Me-3, X = O;) and III·2HCl] and normobaric hypoxia [compounds I·HCl (R1 = Pr-i, R2 = H, Me-2, X = S) and II·HCl] and exceeded bemithylym (33.5 mg/kg) by their activity. The compounds synthesized are low toxic with the LD50 value of 150-250 mg/kg. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Quality Control of 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one).
5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Quality Control of 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia