Tag: M.W=150-200

Nakayama, Chikao published the artcileSynthetic nucleosides and nucleotides. XII. Synthesis and antiviral activities of several 1-β-D-arabinofuranosyl-5-alkyluracils and their 5′-monophosphates, HPLC of Formula: 19030-75-2, the main research area is arabinofuranosylalkyluracil preparation virucide; nucleoside arabinofuranosylalkyluracil; nucleotide arabinofuranosylalkyluracil; uracil arabinofuranosylalkyl.

Arabinofuranosyluracils I (R = Me, Et, Pr, Bu) were prepared by acid hydrolysis of anhydronucleosides II. II were prepared from pyrimidines III by 2 routes : (a) condensation with 1,2-di-O-acetyl-3-O-p-toluenesulfonyl-5-O-benzoyl-D-xylofuranose and treatment of the products with MeONa-MeOH; (b) condensation with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose followed by debenzoylation and cyclization. Phosphorylation of I (R = Me, Et) or II (R = Me, Et) with tetrachloropyrophosphate in MeCn followed by treatment with acid gave 1-β-D-arabinofuranosyl-5-alkyluracil 5′-phosphates (IV). Antiviral activities of I, II, and IV against herpes simplex 1 and 2 are given; I (R = Me) and IV (R = Me) were significantly active against both the viruses.

Journal of Carbohydrates, Nucleosides, Nucleotides published new progress about Antiviral agents. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, HPLC of Formula: 19030-75-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kulikowski, Tadeusz published the artcile5-Substituted arabinofuranosyluracil nucleosides: synthesis and antiviral properties, Recommanded Product: 5-N-Propyluracil, the main research area is arabinofuranosyluracil nucleoside preparation virucide; alkyluracil arabinofuranosyl; structure antiviral activity arabinofuranosyluracil.

The title nucleosides I (R = Et, Pr, Me2CH, Bu), their α-anomers and N-3 isomers were prepared by a number of different procedures based on the catalytic condensation of the corresponding 5-alkyl-2,4-bis(trimethylsilyloxy)pyrimidines with 2,3,5-tri-O-benzyl-α-D-arabinofuranosyl chloride. The resulting protected nucleosides were deblocked by a new procedure based on the use of BF3.Et2O and EtSH. The chloromercuri derivative of ara-U (I; R = H) on reaction with allyl chloride in the presence of Li2PdCl4 gave I (R = allyl), which on catalytic hydrogenation gave I (R = Pr). The antiviral activities of these compounds were evaluated. I (R = allyl) showed moderate specific activity against herpes simplex type 1 virus in PRK cell culture. Structure-activity relationships are discussed.

Acta Biochimica Polonica published new progress about Antiviral agents. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Recommanded Product: 5-N-Propyluracil.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Gadhachanda, Venkat R. published the artcile4-Aminopyrimidines as novel HIV-1 inhibitors, Application of 4-Chloro-6-(methoxymethyl)pyrimidine, the main research area is aminopyrimidine preparation HIV1 inhibitor SAR.

A series of 4-aminopyrimidines was identified as novel HIV inhibitors of unknown mol. target. Structural modifications were carried out to establish SAR and identify the linking site for target identification. A number of analogs were found to possess single digit inhibitory activity for HIV replication. Several analogs with various potential linkers, including a biotinated analog, also exhibited excellent potency, and could serve as tools for the identification of novel anti-HIV targets.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-HIV agents. 3122-84-7 belongs to class pyrimidines, name is 4-Chloro-6-(methoxymethyl)pyrimidine, and the molecular formula is C6H7ClN2O, Application of 4-Chloro-6-(methoxymethyl)pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kawasuji, Takashi published the artcileA platform for designing HIV integrase inhibitors. 2-Hydroxy-3-heteroaryl acrylic acid derivatives as novel HIV integrase inhibitor and modeling of hydrophilic and hydrophobic pharmacophores, Formula: C7H8N2O2, the main research area is hydroxyheteroaryl acrylic acid derivative preparation HIV1 integrase inhibitor antiaids.

The authors present a novel series of HIV integrase inhibitors, showing IC50s ranging from 0.01 to over 370 μM in an enzymic assay. Furthermore, pharmacophore modeling study for the inhibitors was carried out to elucidate the structure-activity relationships. Finally, the authors found a 3D-pharmacophore model, which is composed of a hydrophilic and a hydrophobic domain, providing valuable information for designing other novel types of integrase inhibitors.

Bioorganic & Medicinal Chemistry published new progress about Anti-HIV agents. 42839-08-7 belongs to class pyrimidines, name is Ethyl pyrimidine-2-carboxylate, and the molecular formula is C7H8N2O2, Formula: C7H8N2O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Herstad, Gunnar published the artcileDecarboxylation in the synthesis of 4-alkyl-, 4-alkenyl- and 4-acylpyrimidines, Product Details of C5H5ClN2S, the main research area is pyrimidine alkyl alkenyl acyl preparation decarboxylation carboxypyrimidine; microwave irradiation decarboxylation pyrimidine preparation.

Decarboxylation of allylic esters I (R = H, Me, n = 0; R = Me, n = 2) of 4-carboxypyrimidines in toluene at 111 °C in the presence of a Pd(0) catalyst, tetrakis(triphenylphosphine) palladium, gives a mixture of a 4-alkenylpyrimidine II and a pyrimidine unsubstituted in the 4-position. If the decarboxylation is carried out in the presence of benzaldehyde, then benzaldehyde is added to the 4-position. Decarboxylation of 4-carboxypyrimidines I in the presence of different electrophiles, benzaldehyde, acetophenone and benzoyl chloride, results in incorporation of the electrophile into the 4-position, III [R = CH(OH)Ph, CMe(Ph)(OH), COPh, X = Cl; R = CH(OH)Ph, X = Br], together with a pyrimidine unsubstituted in the 4-position. Use of microwave irradiation enhances the rate of the decarboxylations.

Journal of Heterocyclic Chemistry published new progress about Decarboxylation. 38275-42-2 belongs to class pyrimidines, name is 5-Chloro-2-(methylthio)pyrimidine, and the molecular formula is C5H5ClN2S, Product Details of C5H5ClN2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Iltzsch, Max H. published the artcileStructure-activity relationship of nucleobase ligands of uridine phosphorylase from Toxoplasma gondii, HPLC of Formula: 19030-75-2, the main research area is pyrimidine base Toxoplasma uridine phosphorylase inhibition; structure uracil analog uridine phosphorylase inhibition.

Seventy-nine nucleobase analogs were evaluated as potential inhibitors of T. gondii uridine phosphorylase (UrdPase), and the apparent Ki (appKi) values for these compounds were determined Based on the inhibition data, a structure-activity relationship for the binding of nucleobase analogs to the enzyme was formulated, using uracil as a reference compound Two compounds were identified as very potent inhibitors of T. gondii UrdPase: 5-benzyloxybenzylbarbituric acid and 5-benzyloxybenzyluracil, which had appKi values of 0.32 and 2.5 μM, resp. A comparison of the results from the present study with those from similar studies on mammalian UrdPase and thymidine phosphorylase (dThdPase) revealed that there are both similarities and differences between the catalytic site of T. gondii UrdPase and the catalytic sites of the mammalian enzymes with respect to binding of uracil analogs. One compound, 6-benzyl-2-thiouracil, was identified as a potent, specific inhibitor (appKi = 14 μM) of T. gondii UrdPase, relative to mammalian UrdPase and dThdPase.

Biochemical Pharmacology published new progress about Enzyme kinetics. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, HPLC of Formula: 19030-75-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Miazga, Agnieszka published the artcileSynthesis and anti-HIV properties of novel 6-phenylselenenyl-5-propyluracils, Computed Properties of 19030-75-2, the main research area is phenylselenenylpropyluracil preparation antiHIV antiviral antiHIV antiAIDS.

Novel 6-phenylselenenyl-5-propyluracils were synthesized from 5-propyluracil with the use of regioselective synthesis to give 1-[(2-hydroxyethoxy)methyl]-6-phenylselenenyl-5-propyluracil (6), 1-ethoxymethyl-6-phenylselenenyl-5-propyluracil (9) and 1-benzyloxymethyl-6-phenylselenenyl-5-propyluracil (10). Interaction of these compounds with recombinant HIV-1 reverse transcriptase (RT) was evaluated using a non-isotopic colorimetric method. Compounds 9 and 10 exerted potent HIV RT inhibition (IC50 = 0.06 and 0.05 μM resp.) while compound 6 showed moderate inhibition (IC50 = 3.5 μM). Potent anti-HIV-1 activity in MT-2 cells inoculated by a syncythia-inducing HIV-1 (cat #3 strain) laboratory isolate was exerted by compounds 9 and 10 (EC50 = 0.62 μM and 0.025 μM, resp.), while compound 6 showed only moderate activity (IC50 = 4.1 μM). In addition, compound 10 showed very good in vitro therapeutic index (TI > 2046), indicating that it is a potential anti-HIV/AIDS drug.

Acta Biochimica Polonica published new progress about AIDS (disease). 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Computed Properties of 19030-75-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sturala, Jiri published the artcileElectron-Deficient Heteroarenium Salts: An Organocatalytic Tool for Activation of Hydrogen Peroxide in Oxidations, SDS of cas: 42839-08-7, the main research area is heteroarenium salt organocatalytic activation hydrogen peroxide oxidations.

A series of monosubstituted pyrimidinium and pyrazinium triflates and 3,5-disubstituted pyridinium triflates were prepared and tested as simple catalysts of oxidations with hydrogen peroxide, using sulfoxidation as a model reaction. Their catalytic efficiency strongly depends on the type of substituent and is remarkable for derivatives with an electron-withdrawing group, showing reactivity comparable to that of flavinium salts which are the prominent organocatalysts for oxygenations. Because of their high stability and good accessibility, 4-(trifluoromethyl)pyrimidinium and 3,5-dinitropyridinium triflates are the catalysts of choice and were shown to catalyze oxidation of aliphatic and aromatic sulfides to sulfoxides, giving quant. conversions, high preparative yields and excellent chemoselectivity. The high efficiency of electron-poor heteroarenium salts is rationalized by their ability to readily form adducts with nucleophiles, as documented by low pKR+ values (pKR+ < 5) and less neg. reduction potentials (Ered > -0.5 V). Hydrogen peroxide adducts formed in situ during catalytic oxidation act as substrate oxidizing agents. The Gibbs free energies of oxygen transfer from these heterocyclic hydroperoxides to thioanisole, obtained by calculations at the B3LYP/6-311++g(d,p) level, showed that they are much stronger oxidizing agents than alkyl hydroperoxides and in some cases are almost comparable to derivatives of flavin hydroperoxide acting as oxidizing agents in monooxygenases.

Journal of Organic Chemistry published new progress about Activation energy. 42839-08-7 belongs to class pyrimidines, name is Ethyl pyrimidine-2-carboxylate, and the molecular formula is C7H8N2O2, SDS of cas: 42839-08-7.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Henriksen, Ulla published the artcileFacile synthesis of N-(1-alkenyl) derivatives of 2,4-pyrimidinediones, Application In Synthesis of 19030-75-2, the main research area is pyrimidinedione alkenyl derivative synthesis.

N-(1-alkenyl) derivatives of 2,4-pyrimidinediones were prepared in a one pot synthesis from aldehydes and the nucleobases using trimethylsilyl trifluoromethanesulfonate (TfOTMS) as coupling reagent. Presilylation of the above nucleobases, and N6-benzoyladenine, with excess N,O-bis(trimethylsilyl)acetamide (BSA) followed by addition of one mol eq. TfOTMS yielded the N-(1-trimethylsilyloxyalkyl) derivatives

Nucleosides, Nucleotides & Nucleic Acids published new progress about Coupling reaction. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Application In Synthesis of 19030-75-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sandosham, Jessie published the artcileSyntheses of 5-alkenylpyrimidines by organotin reactions, HPLC of Formula: 84755-30-6, the main research area is stannylpyrimidine preparation coupling alkenyl bromide; vinylpyrimidine; alkenylpyrimidine; halopyrimidine coupling vinyltin; pyrimidine alkenyl.

5-Stannylpyrimidine I (R = SnBu3) (II) was prepared from I (R = Br) by lithiation at -95° and quenching with Bu3SnCl. II is used in Pd-catalyzed coupling reactions with vinyl bromides to give 5-vinylpyrimidines I (R = CH:CHR1, R1 = H, Me, Ph). The opposite reaction sequence, i.e. Pd-catalyzed coupling between 5-halopyrimidines and vinyltin derivatives, is also described. Alternatively, the 5-vinylpyrimidines have been obtained by dehydrohalogenation with CsF and by a modified Wittig reaction. 2-Methylthiopyrimidines are transformed into the 2-methoxy derivatives or 2-pyrimidinones using chloramine-T in a simple one-pot synthesis.

Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry published new progress about Coupling reaction. 84755-30-6 belongs to class pyrimidines, name is 4-Methyl-2-(methylthio)pyrimidine-5-carbaldehyde, and the molecular formula is C7H8N2OS, HPLC of Formula: 84755-30-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia