Tag: M.W=150-200

Rabal, Obdulia; Sanchez-Arias, Juan A.; Cuadrado-Tejedor, Mar; de Miguel, Irene; Perez-Gonzalez, Marta; Garcia-Barroso, Carolina; Ugarte, Ana; Estella-Hermoso de Mendoza, Ander; Saez, Elena; Espelosin, Maria; Ursua, Susana; Haizhong, Tan; Wei, Wu; Musheng, Xu; Garcia-Osta, Ana; Oyarzabal, Julen published the artcile< Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease>, Application In Synthesis of 89793-12-4, the main research area is histone deacetylase HDAC phosphodiesterase PDE5 inhibitor antialzheimer Alzheimer.

Simultaneous inhibition of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) has recently been validated as a potentially novel therapeutic approach for Alzheimer’s Disease (AD). To further extend this concept, the authors designed and synthesized the first chem. series of dual acting PDE5 and HDAC inhibitors, and the authors validated this systems therapeutics approach. Following the implementation of structure- and knowledge-based approaches, initial hits were designed and were shown to validate the hypothesis of dual in vitro inhibition. Then, an optimization strategy was pursued to obtain a proper tool compound for in vivo testing in AD models. Initial hits were translated into mols. with adequate cellular functional responses (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation in the nanomolar range), an acceptable therapeutic window (>1 log unit) and the ability to cross the blood-brain barrier, leading to the identification of 7 as a candidate for in vivo proof-of-concept testing.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Application In Synthesis of 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Law, Robert P.; Ukuser, Sabri; Tape, Daniel T.; Talbot, Eric P. A. published the artcile< Regioselective Synthesis of 3-Aminoimidazo[1,2-a]pyrimidines with Triflic Anhydride>, Electric Literature of 89793-12-4, the main research area is regioselective synthesis aminoimidazopyrimidine cyclization pyrimidine amide triflic anhydride pyridine.

The regioselective synthesis of 3-aminoimidazo[1,2- a]pyrimidines via triflic anhydride mediated amide activation and intramol. cyclization is reported. The nature of the added pyridine base allows access to both regioisomers from a simple common precursor [e.g., treatment of pyrimidine amide I with Tf2O and pyridine bases yielded II + III (yield ratios 8:45 % using 2,6-difluoropyridine and 83:9 % using 2-fluoropyridine)]. The method tolerates a range of functional groups and provides access to novel heterocyclic scaffolds.

Synthesis published new progress about Cyclization catalysts (regioselective). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Electric Literature of 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Bretschneider, H.; Kloetzer, W.; Spiteller, G.; Dehler, J. published the artcile< New pyrimidines and their conversion into 6-sulfanilamidopyrimidines. Preliminary communications>, HPLC of Formula: 3286-55-3, the main research area is .

The favorable chemotherapeutic properties of 6-sulfanilamido-2,4-dimethoxypyrimidine (I) motivated the preparation of a number of 2,4-disubstituted 6-sulfanilamidopyrimidines. From II were prepared the following IIa (R, R’, and R” given): MeO, MeO, Cl (III); MeO, MeO, NMe3Cl; MeO, Cl, Cl (IV); MeO, MeO, EtS; MeO, MeO, EtSO2; MeO, MeO, PhS; MeO, MeO, PhSO2; MeO, MeO, 4-AcNHC6H4SO2; Cl, Cl, NH2; MeO, MeO, NH2; EtS, EtS, NH2; CH2:CHCH2O, CH2:CHCH2O, NH2 (V); MeOCH2CH2O, MeOCH2CH2O, NH2; MeO, Cl, NH2; EtS, Cl, NH2; MeO, H, NH2; MeO, EtS, NH2; EtS, MeO, NH2. Also prepared was Va. Two procedures were used to introduce the sulfanilamido group: (1) replacement of the 6-substituent by treatment with 4-H2NC6H4SO2NHNa (VI) or 4-AcNHC6H4SO2NHNa (VII) and (2) the standard acylation with an N4-acylaminobenzenesulfonyl chloride in pyridine followed by hydrolysis. Treatment of II with VII gave (VIII) (R” = Ac, R’ = R = Cl), converted by acid hydrolysis to VIII (R” = H, R’ = R = Cl) (IX). Partial methanolysis of IX with NaOMe gave VIII (R” = H, R’ = Cl, R = OMe) (X) and total methanolysis afforded I. X was also prepared from IV and VII to give VIII (R” = Ac, R’ = Cl, R = OMe) (XI), followed by hydrolysis. Methanolysis of XI followed by hydrolysis gave I. X treated with Me2NH gave VIII (R” = H, R’ = NMe2, R = OMe). I was also obtained from III and VI, and X from IV and VI. V was converted to VIII (R” = Ac, R’ = R = OCH2CH2OMe) and hydrolyzed to VIII (R = H, R’ = R = OCH2CH2OMe). The following VIII (R” = EtO2C) were reported (R and R’ given): MeO, MeO; EtS, EtS; CH2:CHCH2O, CH2:CHCH2O; MeO, EtS; EtS, MeO. Also prepared was XII. Hydrolysis of the above compounds gave the corresponding sulfapyrimidines. Complete details of this work are in preparation

Monatshefte fuer Chemie published new progress about 3286-55-3. 3286-55-3 belongs to class pyrimidines, and the molecular formula is C5H6ClN3O, HPLC of Formula: 3286-55-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hornillo-Araujo, Ana R.; Burrell, Adam J. M.; Aiertza, Miren K.; Shibata, Takayuki; Hammond, David M.; Edmont, Dolores; Adams, Harry; Margison, Geoffrey P.; Williams, David M. published the artcile< The syntheses and properties of tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine and O6-methylguanine>, Formula: C7H8N4O, the main research area is tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; thiopyran tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; thiepane tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; DNA cross linking tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; oligonucleotide pseudosubstrate DNA linking tricyclic pyrrolopyrimidine analog thioguanine methylguanine.

The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogs of S6-methylthioguanine are described. The crystal structures and pKa values of these and related O6-methylguanine analogs are reported. All compounds display higher pKa values than O6-methylguanine with the sulfur-containing analogs being the more basic and exhibiting higher stability in aqueous solution In a standard substrate assay with the human repair protein O6-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analog displayed activity.

Organic & Biomolecular Chemistry published new progress about Crystal structure. 84955-32-8 belongs to class pyrimidines, and the molecular formula is C7H8N4O, Formula: C7H8N4O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Amano, Yohei; Noguchi, Masayuki; Shudo, Koichi published the artcile< Diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as retinoid X receptor (RXR)-specific agonists>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is arylamino hexahydro phenalene preparation retinoid X receptor agonist; octahydro benzoheptalene arylamino preparation retinoid X receptor agonist.

A series of diarylamines I (X = CH2, R1 = H, Me; X = CH2CH2, R1 = H; Z = CH, N; R2 = H, Me, Et, cyclopropylmethyl, i-Bu, PhCH2) incorporating hexahydrophenalene or octahydrobenzoheptalene as a hydrophobic moiety was synthesized and examined for their activities towards retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Most of these compounds showed agonistic activity towards RXRs, but were inactive towards RARs. These RXR-specific ligands showed synergistic activity in RARα,β ligand-induced terminal differentiation of leukemia cell line HL-60.

Chemical & Pharmaceutical Bulletin published new progress about Aromatic amines Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Okui, Kiyoshi; Ito, Kiyohiko; Koizumi, Masuo; Fukumoto, Keiichiro; Kametani, Tetsuji published the artcile< Syntheses of heterocyclic compounds. CDXCI. Pyrimidine derivatives. V. Abnormal condensation products of 4-amino-6-chloro-2-methoxypyrimidine with p-nitrobenzenesulfonyl chloride>, Related Products of 3286-55-3, the main research area is pyridinium pyrimidine betaines.

Condensation of 4-amino-6-chloro-2-methoxypyrimidine with p-O2NC6H4SO2Cl gave, in addition to 6-chloro-2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidine (I), two abnormal by-products, 1-[2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidin-6-yl]pyridinium N,N-betaine (II) and N-(p-nitrobenzenesulfonyl)-β-ureido-β-pyridinium arcylamide N,N-betaine (III).

Journal of Heterocyclic Chemistry published new progress about 3286-55-3. 3286-55-3 belongs to class pyrimidines, and the molecular formula is C5H6ClN3O, Related Products of 3286-55-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Park, Tae-Hong; Cychosz, Katie A.; Wong-Foy, Antek G.; Dailly, Anne; Matzger, Adam J. published the artcile< Gas and liquid phase adsorption in isostructural Cu3[biaryltricarboxylate]2 microporous coordination polymers>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is gas liquid adsorption copper isostructural biaryltricarboxylate microporous polymer; crystal structure copper carboxypyrimidinyl carboxypyridinyl isophthalate microporous coordination polymer; copper biaryltricarboxylate microporous polymer preparation gas liquid adsorption.

N-Heteroarene substitution in biphenyl-based linkers enhances the uptake of electron-rich organosulfur mols. in microporous coordination polymers (MCP). Three isostructural MCPs are prepared (Cu3L2) possessing nearly uniform surface areas from homologous biaryl tricarboxylate linkers containing Ph (biphenyltricarboxylate UMCM-150), pyrimidine (carboxypyrimidinyl-isophthalate UMCM-150N2), and pyridine (carboxypyridinyl-isophthalate UMCM-150N1) units, building the ideal system to probe linker influence upon guest adsorption. The almost identical isotherms of H2 and CO2 in these MCPs imply that the N-heteroaryl linkers in the UMCM-150 analogs do not considerably affect the gas phase adsorption behavior. The electronic nature and contact interactions with the aromatic linker play an important role to enhance interactions between the host MCP framework and the large guest organic mols. in the liquid phase.

Chemical Communications (Cambridge, United Kingdom) published new progress about Adsorption (isotherm). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia