Category: 39083-15-3

Isocytosine H₂-receptor histamine antagonists. I. Oxmetidine and related compounds was written by Brown, Thomas H.;Blakemore, Robert C.;Durant, Graham J.;Emmett, John C.;Ganellin, C. Robin;Parsons, Michael E.;Rawlings, D. Anthony;Walker, Terence F.. And the article was included in European Journal of Medicinal Chemistry in 1988.Quality Control of 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one The following contents are mentioned in the article:

2-[2-(5-Methyl-4-imidazolylmethylthio)ethylamino]-4-pyrimidones I (R = H, Me, PhO, substituted benzyl, etc.; R¹ = H, Me, Pr, PhCH₂) were prepared via substitution of (methylthio)pyrimidinones with 5-methyl-4-[(2-aminomethyl)thiomethyl]imidazole. The model compound I (R = R¹ = H) has modest H₂-antagonist activity as shown by its ability to antagonize histamine-stimulated tachycardia in guinea pig right atrium in vitro and inhibit histamine-stimulated gastric acid secretion in the lumen-perfused stomach of the anesthetized rat. Investigation of the effect of substituents in the pyrimidone ring showed that suitable substitution at the 5-position gave compounds with greatly increased activity, whereas substituents at other positions in the ring were not favorable for activity. Some structure-activity and structure-toxicity correlations are discussed. 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. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Quality Control of 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hydrazones based on 5-ethyl-4-methyl-2-thiouracil was written by Vainilavicius, P.;Jasinskas, L.;Kuznecovaite, V.;Kimtys, L.. And the article was included in Liet. TSR Aukst. Mokyklu Mokslo Darb., Chem. Chem. Technol. in 1972.Recommanded Product: 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one The following contents are mentioned in the article:

R1COCH2Br (0.11 mole) was added to a refluxing mixture of 0.1 mole 4-(ethylthio)- or 2-thio-5-ethyl-6-methyluracil, and the mixture refluxed 4-5 hr to give the following I (R, R1, Z, and % yield given): OH, Ph, S, 60; OH, m-O2NC6H4, S, 67; EtS, Ph, O, 40; and EtS, m-O2NC6H4, O, 40. I (0.02 mole) and 0.032 mole R2CONHNH2 in MeOH refluxed 12-25 hr, then kept 12 hr at 0° gave the following II (R, R1, R2, Z, and % yield given): OH, Ph, Ph, S, 90; OH, Ph, m-O2NC6H4, S, 74; OH, Ph, ο-HOC6H4, S, 67; OH, Ph, m-HOC6H4, S, 83; OH, p-HOC6H4, Ph, S, 59; OH, Ph, p-H2NC6H4, S, 57; OH, Me, Ph, S, 65; OH, m-O2NC6H4, Ph, S, 63; OH, m-O2NC6H4, m-O2NC6H4, S, 44; OH, m-O2NC6H4, ο-HOC6H4, S, 50; OH, m-O2NC6H4, m-HOC6H4, S, 50; OH, m-O2NC6H4, p-HOC6H4, S, 50; OH, m-O2NC6H4, Me, S, 54; EtS, Ph, Ph, O, 40; EtS, Ph, m-O2NC6H4, O, 59; EtS, Ph, p-HOC6H4, O, 54; EtS, Ph, m-O2NC6H4, O, 60; EtS, m-O2NC6H4, m-O2NC6H4, O, 32; and EtS, m-O2NC6H4, p-HOC6H4, O, 36. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Recommanded Product: 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. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. 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.Recommanded Product: 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and evaluation of 5,6-disubstituted thiopyrimidine aryl aminothiazoles as inhibitors of the calcium-activated chloride channel TMEM16A/Ano1 was written by Piechowicz, Katarzyna A.;Truong, Eric C.;Javed, Kashif M.;Chaney, Rachelle R.;Wu, Johnny Y.;Phuan, Puay W.;Verkman, Alan S.;Anderson, Marc O.. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2016.COA of Formula: C7H10N2OS The following contents are mentioned in the article:

Transmembrane protein 16A (TMEM16A), also called Ano1, is a Ca²⁺ activated Cl^– channel expressed widely in mammalian epithelia, as well as in vascular smooth muscle and some tumors and elec. excitable cells. TMEM16A inhibitors have potential utility for treatment of disorders of epithelial fluid and mucus secretion, hypertension, some cancers and other diseases. 4-Aryl-2-amino thiazole was previously identified by high-throughput screening. Here, a library of 47 compounds were prepared that explored the 5,6-disubstituted pyrimidine scaffold found in. TMEM16A inhibition activity was measured using fluorescence plate reader and short-circuit current assays. The authors found that very little structural variation of was tolerated, with most compounds showing no activity at 10 渭M. The most potent compound in the series, which substitutes 4-methoxyphenyl in with 2-thiophene, had IC₅₀ éˆ? 渭M for inhibition of TMEM16A chloride conductance. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3COA of Formula: C7H10N2OS).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.COA of Formula: C7H10N2OS

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and evaluation of 5,6-disubstituted thiopyrimidine aryl aminothiazoles as inhibitors of the calcium-activated chloride channel TMEM16A/Ano1 was written by Piechowicz, Katarzyna A.;Truong, Eric C.;Javed, Kashif M.;Chaney, Rachelle R.;Wu, Johnny Y.;Phuan, Puay W.;Verkman, Alan S.;Anderson, Marc O.. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2016.COA of Formula: C7H10N2OS The following contents are mentioned in the article:

Transmembrane protein 16A (TMEM16A), also called Ano1, is a Ca²⁺ activated Cl^– channel expressed widely in mammalian epithelia, as well as in vascular smooth muscle and some tumors and elec. excitable cells. TMEM16A inhibitors have potential utility for treatment of disorders of epithelial fluid and mucus secretion, hypertension, some cancers and other diseases. 4-Aryl-2-amino thiazole was previously identified by high-throughput screening. Here, a library of 47 compounds were prepared that explored the 5,6-disubstituted pyrimidine scaffold found in. TMEM16A inhibition activity was measured using fluorescence plate reader and short-circuit current assays. The authors found that very little structural variation of was tolerated, with most compounds showing no activity at 10 渭M. The most potent compound in the series, which substitutes 4-methoxyphenyl in with 2-thiophene, had IC₅₀ 鈭? 渭M for inhibition of TMEM16A chloride conductance. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3COA of Formula: C7H10N2OS).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.COA of Formula: C7H10N2OS

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidines. LXIV. Synthesis of 4-Methyl-5-ethyleytosine was written by Johnson, Treat B.;Bailey, George C.. And the article was included in Journal of the American Chemical Society in 1913.Application of 39083-15-3 The following contents are mentioned in the article:

2-Thio-4-methyl-5-ethyl-6-oxypyrimidine, from CS(NH₂)₂, AcCHEtCO₂Et and Na in alc. 3-4 hrs. on the H₂O bath, prisms, m. 212° (yield, 60%); its Na. salt in alc. gives with PhCH₂Cl the 2-benzyltnercapto derivative, blocks, m. 160°; 2-ethylmercapto derivative, m. 138°, converted by PCl₆ at 100° after 10-12 hrs. into 2-ethylmercapto-4-methyl-5-ethyl-6-chloropyrimidine, b_23-1 177-80°, and by PhNH₂ in hot alc. into 2-anilino-4-methyl-5-ethyl-6-oxypyrimidine, m. 195°, while alc. NH₃, 3 hrs. at 150-60, instead of PhNH₂ gives the 2-amino compound, Minute Prisms, m. 281-20 (decompose); hydrobromide, needles, m. 160-75°, depending on the rate of heating; hydrochloride, apparently seps. with 1 H₂O, shrivels 80°, m. 11.5°. 2-Ethylmercapto-4-methyl-5-etlzyl-6-aminopyrimidine, from the above 6-Cl compound and alc. NH₃ at 140-50°, stout blocks, m. 89-91°, hydrolyzed by b. concentrate HCl to the hydrochloride, powder, decompose 125°, of 2-oxy-4-methyl-5-ethyl-6-aminopyrimidine (methylethylcylosine), blocks or rectangular prisms, m. 295° (decompose); hydrobromide, blocks, dedomp. about 260°. 4-Methyl-5-ethyluracil is obtained quant. by b. 2-ethylmereapto-4-methyl-5-ethyl-6-oxypyrimidine with 2 parts of ClCH₂CO₂H in H₂O. 2-Diphenylmethylmercapto-4-methyl-6-oxypyrimidine, from Ph₂CHBr, 2-thio-4-methyluracil and Na in alc., m. 214. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Application of 39083-15-3).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. 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.Application of 39083-15-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

An Antiparasitic Compound from the Medicines for Malaria Venture Pathogen Box Promotes Leishmania Tubulin Polymerization was written by Ullah, Imran;Gahalawat, Suraksha;Booshehri, Laela M.;Niederstrasser, Hanspeter;Majumdar, Shreoshi;Leija, Christopher;Bradford, James M.;Hu, Bin;Ready, Joseph M.;Wetzel, Dawn M.. And the article was included in ACS Infectious Diseases in 2020.Reference of 39083-15-3 The following contents are mentioned in the article:

The few frontline antileishmanial drugs are poorly effective and toxic. To search for new drugs for this neglected tropical disease, we tested the activity of compounds in the Medicines for Malaria Venture (MMV) “Pathogen Box” against Leishmania amazonensis axenic amastigotes. Screening yielded six discovery antileishmanial compounds with EC₅₀ values from 50 to 480 nM. Concentration-response assays demonstrated that the best hit, MMV676477(I), had mid-nanomolar cytocidal potency against intracellular Leishmania amastigotes, Trypanosoma brucei, and Plasmodium falciparum, suggesting broad antiparasitic activity. We explored structure-activity relationships (SAR) within a small group of MMV676477 analogs and observed a wide potency range (20-5000 nM) against axenic Leishmania amastigotes. Compared to MMV676477, our most potent analog, SW41, had ~5-fold improved antileishmanial potency. Multiple lines of evidence suggest that MMV676477 selectively disrupts Leishmania tubulin dynamics. Morphol. studies indicated that MMV676477 and analogs affected L. amazonensis during cell division. Differential centrifugation showed that MMV676477 promoted partitioning of cellular tubulin toward the polymeric form in parasites. Turbidity assays with purified Leishmania and porcine tubulin demonstrated that MMV676477 promoted leishmanial tubulin polymerization in a concentration-dependent manner. Analogs’ antiparasitic activity correlated with their ability to facilitate purified Leishmania tubulin polymerization Chem. crosslinking demonstrated binding of the MMV676477 scaffold to purified Leishmania tubulin, and competition studies established a correlation between binding and antileishmanial activity. Our studies demonstrate that MMV676477 is a potent antiparasitic compound that preferentially promotes Leishmania microtubule polymerization Due to its selectivity for and broad-spectrum activity against multiple parasites, this scaffold shows promise for antiparasitic drug development. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Reference of 39083-15-3).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Reference of 39083-15-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Some thiopyrimidine derivatives was written by Monti, Lydia;Pacini, Carlo. And the article was included in Gazzetta Chimica Italiana in 1948.Product Details of 39083-15-3 The following contents are mentioned in the article:

By the reaction of HCHO (I), in the presence of H₂SO₄, on thiopyrimidines of the HN.CO.CH:CR.NH.CS ⇄ N:C(OH).CH:CR.N:CSH (II) and HN.CO.CR’:CMe.NH.CS ⇄ N:C(OH).CR’:CMe.N:CSH (III) types, 2 series of new derivatives were obtained. They are essentially different from those prepared by Kircher (C.A. 6, 857) and Poetsch and Behrend (C.A. 20, 2681) by the action of I on HN.CO.CH:CMe.NH.CO and HN.CO.CH:CMe.NH.CS, resp., in acid medium. With II the reactions involve the initial reaction of I with enolic II in the 5-position, following which another I mol. reacts with the newly formed OH group and the original OH group in the 6-position, with final formation of compounds of the C:CR.N:C(SH).N:C.O.CH₂.O.CH₂ (IV) type. With III, in which the H in the 5-position is replaced by an alkyl group, the formation of analogous compounds is difficult to explain, for no intermediate products could be isolated. Perhaps I reacts with III in the ketone-imide form with formation of SC.N.CO.CR’:CMe.N.CH₂.O.CH₂ compounds If so, 1,3-dimethylol compounds would be intermediate products, but none was isolated. Possibly the NH group in the 1-position (between CS and CO) is more reactive than that in the 3-position, and SC.N.CH₂.O.CH₂.O.C:CR’.CMe:N or S.CH₂.O.CH₂.N.CO.CR’:CMe.N:C compounds are formed. Or III compounds may react in a tautomeric form N:C(OH).CHR’.CMe:N.CS, with formation of N:C.O.CH₂.O.CH₂.CR’.CMe:N.CS compounds Comparative physiol. tests of these doubtful compounds and of II, III, and IV now in progress may help solve this problem. (H₂N)₂CS (2.5 g.), 6 g. AcAmCHCO₂Et, and alc. NaOEt (from 1.5 g. Na in a min. of EtOH), refluxed 30-40 min., evaporated, the residue taken up in AcOH (60 cc. AcOH + 40 cc. water), filtered, and the product purified by water, yield 60% of 4-methyl-5-amyl-2-thiouracil (V), m. 217-19°, soluble in dilute aqueous alkalies, and decomposed by boiling concentrated aqueous alkalies (evolution of H₂S and NH₃). It behaves like a weak monobasic acid. With aqueous AgNO₃, its boiling concentrated aqueous solutions deposit the Ag salt, C₁₀H₁₅ON₂SAg. The Cu and Hg salts were prepared similarly. 4-Phenyl-2-thiouracil (IV) (2 g.) in 15 cc. hot 10% aqueous NaOH, allowed to stand 24 hrs. with 4 cc. 40% I, diluted, neutralized with dilute HCl, and the precipitate purified by EtOH, yields 86% 5-(hydroxymethyl)-4-phenyl-2-thiouracil (VII), m. 250-1°, evolves I when heated; its solutions in concentrated H₂SO₄ are intensely yellow. 4-Methyl-2-thiouracil (2 g.), 16 cc. dilute H₂SO₄ (4 volumes concentrated H₂SO₄ + 1 volume water), and 3 cc. 40% I, allowed to stand 24 hrs. (with frequent agitation), diluted with 100 cc. water, neutralized with NH₄OH, filtered, and the residue purified by boiling water and CCl₄, yield the methylenic ether of 2-thio-4-methyl-6-hydroxy-5-pyrimidinemethanol (VIII), does not form an Ac derivative; its concentrated H₂SO₄ solution with a trace of gallic acid gives the green-to-blue Labat reaction; when heated with a dilute alkali, it evolves H₂S and NH₃. VII and I in dilute H₂SO₄, also under the same conditions, form VIII. VI or VII (3 g.) and 4 cc. 40% I in 16 cc. dilute H₂SO₄ (4 volumes concentrated H₂SO₄ + 1 volume water), treated as above, yield 95% of methylenic ether of 2-thio-4-phenyl-6-hydroxy-5-pyrimidinemethanol, m. 151-2°, yellow when crystallized from EtOH but colorless from CCl₄. It gives a pos. Labat reaction, and is decomposed, with evolution of H₂S and NH₃, by hot dilute alkalies. Prepared under similar conditions from 4,5-dimethyl-2-thiouracil (IX) and I in 73% yield and purified by boiling water, the methylenic ether (X) of IX m. 133-5°, does not give an Ac derivative, gives a pos. Labat reaction, and is decomposed by hot aqueous alkalies with evolution of H₂S and NH₃. 4-Methyl-5-ethyl-2-thiouracil and I give 82-3% of the methylenic ether (XI), m. 163-4°, with chem. properties similar to those of X. V (2 g.) in 22 cc. dilute H₂SO₄ (same concentration as before) and 3 cc. 40% I, allowed to stand 24 hrs., diluted, neutralized with NH₄OH, concentrated, and the product purified by boiling water, yield 41% of the methylenic ether, m. 122-5°, with chem. properties like those of X and XI. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Product Details of 39083-15-3).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Product Details of 39083-15-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Relation between goitrogenic effect and chemical constitution was written by Jensen, K. A.;Kjerulf-Jensen, K.. And the article was included in Acta Pharmacologica et Toxicologica in 1945.Name: 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one The following contents are mentioned in the article:

In young rats, benzenesulfonic acid, phenyl p-toluenesulfonate, p-toluenesulfonamide, taurine, N⁴-(o-carboxybenzoyl)sulfathiazole, Na salt of N⁴-(1-sulfoethyl)sulfathiazole, p-tolyl isothiocyanate, ethylene dithiocyanate, mercaptoacetic acid, cysteine, mercaptosuccinic acid, p-toluenethiol, o-mercaptobenzoic acid, dibenzyl sulfide, bis(2-carboxyethyl) sulfide, α,α’-(thiocarbonyldithio)bis[glycolic acid], thioacetamide, thiobenzamide, xanthogenamide (H₂NC(:S)OEt), Et thionocarbanilate, N-allyl-N’-(m-carboxyphenyl)thiourea, selenourea, 2-methyl-2-thiopseudourea sulfate, thiosemicarbazide, 4-allylthiosemicarbazide, hydrazodithiodicarboxamide, 1,3-oxalylthiourea (thioparabanic acid), 1,3-ethylenethiocarbamide (2-thioxoimidazolidine), 2(3)-benzimidazolethione, 2-imino-4-thiazolidone-5-acetic acid, 5-imino-3-thioxo-1,2,4-dithiazolidine, 2-aminothiazole, thioammeline, 2-amino-4-methyl-6-mercaptopyrimidine, 6-methyl-4-thiouracil, 5-methyl-2-thiouracil (thiothymine), 6-methyluracil, 6-amino-2-thiouracil, 2-amino-4-hydroxy-6-methylpyrimidine, 2-mercapto-4-methyl-6-aminopyrimidine, 2-mercapto-4,6-dimethylpyrimidine, 2-methylmercapto-4-mercapto-6-methylpyrimidine, 2-mercapto-4-phenyl-6-methylpyrimidine, compound (1:1) of NH₃ and 6-imino-5-isonitroso-2-thiouracil, 2-thio-5-aminobarbituric acid (thiouramil), 2-thio-5-ethylbarbituric acid, 2-thioxanthine, 2-thiopseudouric acid, dithiohydurilic acid, 2,4-dioxothiazolidine, 1,4-dithiane, s-trithiane, phenothiazine, biuret, biguanide, dicyandiamidine, thiodicyandiamidine, 1-phenylsemicarbazide, benzoylacetone, salicylaldehyde oxime, β-isatin oxime, dimethylglyoxime, 5-isonitrosobarbituric (violuric) acid, 1-phenyl-3-methyl-4-isonitroso-5-pyrazolone, salicylaldehyde phenylhydrazone, glyoxal osazone, 8-hydroxyquinoline, triphenylphosphine, triphenylarsine, K xanthate, Na diethyldithiocarbamate, KCN, Na₂S, and Na₂S₂O₃ had no goitrogenic action. Sulfaguanidine, sulfonal, dithioöxamide, thiourea, allylthiourea, 1,3-diphenylthiourea, 2-thiohydantoin, 4-oxo-2-thioxo-1,2,3,4-tetrahydroquinazoline, 1,3-(1,8-naphthylene)thiourea, thioantipyrine, and p-aminobenzoic acid were weakly goitrogenic or of doubtful effect. Methylthiourea, trimethylthiourea, tetramethylthiourea, dithizone, 6-methyl-2-thiouracil, 6-methyl-5-ethyl-2-thiouracil, 6-methyl-5-butyl-2-thiouracil (m. 189°, preparation described), 6-methyl-5-isoamyl-2-thiouracil (m. 222-3°, preparation given), and 4-phenyl-2-thiouracil were strongly goitrogenic. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Name: 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. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Name: 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Gadolinium chloride inhibition of rat hepatic microsomal epoxide hydrolase and glutathione S-transferase gene expression was written by Kim, Sang Geon;Choi, Sung Hee. And the article was included in Drug Metabolism and Disposition in 1997.Reference of 39083-15-3 The following contents are mentioned in the article:

The effects of gadolinium chloride, a Kupffer cell toxicant, on the constitutive and inducible expression of hepatic microsomal epoxide hydrolase (mEH) and glutathione S-transferase (GST) genes were examined in rats. Northern blot anal. showed that treatment of rats with GdCl₃ caused suppression of mEH and GST gene expression. MEH mRNA levels were decreased in a time-dependent manner after a single injected dose of GdCl₃ (10 mg/kg, i.v.), resulting in 95, 55, 17, 36, and 69% of the levels in untreated animals at 6, 12, 18, 24, and 48 h after treatment, resp. A maximal reduction in GST Ya, Yb1/2, and Yc1 mRNA levels was also noted at 18 h after treatment with GdCl₃, followed by a gradual return to levels in untreated rats at later time points. Whereas treatment of rats with thiazole, allyl disulfide, Pr sulfide, oltipraz, or clotrimazole caused 2-13-fold increases in mEH mRNA levels at 18 h after treatment, concomitant GdCl₃ treatment caused 30-70% reductions in the increases in mEH mRNA levels. The chem.-inducible mRNA levels for GST Ya, Yb1/2, and Yc1 were also significantly inhibited by GdCl₃ at 18 h after treatment. Rats treated with GdCl₃ (10 mg/kg/day, i.v.) for 3-5 consecutive days exhibited 40-90% decreases in mEH, GST Ya, and GST Yb1/2 mRNA levels, relative to control, whereas the Yc1 mRNA level was suppressed at early times and returned to levels in untreated animals at day 5 after treatment. The mRNA levels for mEH and GST Ya in rats treated daily with both allyl disulfide (25 mg/kg, po) and GdCl₃ for 3 consecutive days were 20-30% of those in rats treated with allyl disulfide alone. Western immunoblotting showed that mEH and GST Ya protein expression was decreased at 1-3 days after consecutive daily treatment with GdCl₃. Whereas treatment of rats with GdCl₃ at a dose of 1 mg/kg suppressed constitutive hepatic mEH gene expression by 85% at 18 h, rats treated with CaCl₂ (10 mg/kg, i.v.) in combination with GdCl₃ (1 mg/kg, i.v.) showed 45% suppression of the mEH mRNA level, compared with untreated animals. GdCl₃-induced suppression was also significantly reversed for GST Ya mRNA by excessive CaCl₂ administration. These results demonstrate that GdCl₃ effectively inhibits constitutive and inducible mEH and GST expression, with decreases in their mRNA levels. GdCl₃ suppression of detoxifying enzyme expression may be associated with its blocking of intracellular Ca²⁺ influx, which affects signaling pathways for the expression of the genes. This study involved multiple reactions and reactants, such as 5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3Reference of 39083-15-3).

5-Ethyl-6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one (cas: 39083-15-3) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Reference of 39083-15-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

[(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