Tag: M.W=150-200

Mirguet, Olivier; Sautet, Stephane; Clement, Catherine-Anne; Toum, Jerome; Donche, Frederic; Marques, Celine; Rondet, Emilie; Pizzonero, Mathieu; Beaufils, Benjamin; Dudit, Yann; Huet, Pascal; Trottet, Lionel; Grondin, Pascal; Brusq, Jean-Marie; Boursier, Eric; Saintillan, Yannick; Nicodeme, Edwige published the artcile< Discovery of Pyridones as Oral AMPK Direct Activators>, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is pyridone AMPK activator diabetes type 2 structure activity preperation; AMPK direct activator; P-gp substrate; pyridone; type 2 diabetes.

AMP-activated protein kinase (AMPK) is an evolutionarily conserved fuel-sensing enzyme that is activated in shortage of energy and suppressed in its surfeit. AMPK activation stimulates fatty acid oxidation, enhances insulin sensitivity, alleviates hyperglycemia and hyperlipidemia, and inhibits proinflammatory changes. Thus, AMPK is a well-received therapeutic target for type 2 diabetes and other metabolic disorders. Here, the authors will report the discovery of pyrrolopyridone derivatives as AMPK direct activators. The authors will illustrate the synthesis and structure-activity relationships of the series as well as some pharmacokinetic results. Some compounds exhibited encouraging oral exposure and were evaluated in a mouse diabetic model. 2-Chloro-7-hydroxy-1-[2′-hydroxy-3′-(methyloxy)-4-biphenylyl]-6-phenyl-1,4-dihydro5H-pyrrolo[3,2-b]pyridin-5-one showed oral activity at 30 mg/kg on blood glucose.

ACS Medicinal Chemistry Letters published new progress about Drug discovery. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yang, Rong; Gu, Guozhang; Tang, Chen; Miao, Zhicheng; Cao, Hongwei; Zou, Guoxiang; Li, Jinchun published the artcile< Super-tough and flame-retardant poly(lactic acid) materials using a phosphorus-containing malic acid-based copolyester by reactive blending>, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate, the main research area is fireproofing polylactic phosphorus malic polyester reactive blending.

It is a great challenge to simultaneously prepare flame-retardant and super-tough poly(lactic acid) (PLA) materials. Herein, we reported a facile approach that PLA reactively blends with phosphorus-containing copolyester. In this paper, a quinary aliphatic copolyester (PPE) containing phosphorus and pendent hydroxyl group was synthesized with sebacic acid, di-Me malate, di-Et phosphite, 1,6-hexanediol, and 1,3-propanediol by polycondensation. Then, flame-retardant and super-tough PLA materials (PLA/PPEU) can be achieved by reactively blending with PPE and hexamethylene diisocyanate. The results showed that the toughness of PLA was significantly enhanced. The maximum notched impact strength is 75.3 kJ/m2 indicated a super toughness performance. Meanwhile, the flame retardance of the PLA was improved obviously. The limited oxygen index (LOI) of PLA increased from 20 to 26%. Moreover, the PLA blends can pass the UL-94 V-0 rating. In addition, both the total heat release and total smoke production of PLA were decreased. The resultant super-tough and flame-retardant PLA materials could be widely applied in elec. and electronic equipment.

Polymer Degradation and Stability published new progress about Chars. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Bouayad-Gervais, Samir; Nielsen, Christian D.-T.; Turksoy, Abdurrahman; Sperger, Theresa; Deckers, Kristina; Schoenebeck, Franziska published the artcile< Access to Cyclic N-Trifluoromethyl Ureas through Photocatalytic Activation of Carbamoyl Azides>, Name: 4-tert-Butylphenylisothiocyanate, the main research area is cyclic trifluoromethyl urea preparation; carbamoyl azide potocatalytic activation.

Mild activation of carbamoyl azides to the corresponding nitrenes using a blue light/[Ir]-catalyzed strategy, which enabled stereospecific access to N-trifluoromethyl imidazolidinones and benzimidazolones was reported. These novel structural motifs proved to be highly robust, allowing their downstream diversification. On the basis of combined computational and exptl. studies, it was proposed that an electron rebound with the excited metal catalyst was undergone, involving a reduction-triggered nitrogen loss, followed by oxidation to the corresponding carbamoyl nitrene and subsequent C-H functionalization.

Journal of the American Chemical Society published new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 19241-24-8 belongs to class esters-buliding-blocks, and the molecular formula is C11H13NS, Name: 4-tert-Butylphenylisothiocyanate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Poisson, Jean-Francois; Normant, Jean F. published the artcile< A configurationally stable alkoxy allenyl zinc reagent, en route to anti-anti vicinal amino diols>, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate, the main research area is vicinal amino diol stereoselective preparation; alkoxy allenyl zinc configurationally stable preparation addition imine.

The reaction of an alkoxyallenyl zinc reagent with benzyl imines derived from lactic and mandelic acids proceeds highly diastereoselectively and leads to 2-amino-1,3-diol derivatives with an anti-anti pattern. Thus, successive treatment of MeOCH2OCH2CCSiMe3 with EtCMeLi and ZnBr2 in THF gave the intermediate allenyl zinc reagent I which reacted with the benzyl imines II (R = Ph, Me) in THF at -70° to give the protected anti-anti-amino alcs. III.

Organic Letters published new progress about Addition reaction, stereoselective. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ghosh, Arun K.; Thompson, Wayne J.; Lee, Hee Yoon; McKee, Sean P.; Munson, Peter M.; Duong, Tien T.; Darke, Paul L.; Zugay, Joan A.; Emini, Emilio A. published the artcile< Cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors>, Application of C6H10O5, the main research area is RO 318959 analog HIV protease inhibitor; cyclic sulfonlane asym synthesis HIV inhibitor; virucide sulfolanyloxycarbonylaminohydroxypropyl isoquinolinamide preparation.

Recently the use of urethanes of 3-tetrahydrofuran as P2-ligands for the S2-substrate binding site of HIV-1 protease was reported. The urethane of (S)-3-hydroxy sulfolane substantially increased the in vitro potency of inhibitors relative to the heterocycle 3-tetrahydrofuran. Furthermore, introduction of a small 2-alkyl group cis to the 3-hydroxyl group of either heterocycle system further enhances enzyme affinity. This is consistent with modeling studies using the x-ray crystal structure of the enzyme-inhibitor complex of THF derived inhibitor I and HIV-1 protease. The cis-2-iso-Pr group thus far offers optimum enhancement of the inhibitory properties of the 3-hydroxysulfolane providing an inhibitor II; for HIV-1, IC50 3 nM; for HIV-219, IC50 17 nM) of comparable in vitro antiviral potency to present clin. candidate (3S,4aS,8aS,2’R,3’S)-N-tert-butyl-2-(2′-hydroxy-4′-phenyl-3′-[[[N-(2-quinolinylcarbonyl)-L-asparaginyl]amino]butyl]-decahydroisoquinoline-3-carboxamide (Ro 31-8959), but of reduced mol. weight due to the exclusion of the P3-quinoline ligand. A stereoselective and general synthetic route to this novel class of ligands in optically pure form was developed.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Application of C6H10O5.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Kim, DaWon; Lee, Jeong Hwa; Kim, Hye Yun; Shin, Jisu; Kim, Kyeonghwan; Lee, Sejin; Park, Jinwoo; Kim, JinIkyon; Kim, YoungSoo published the artcile< Fluorescent indolizine derivative YI-13 detects amyloid-β monomers, dimers, and plaques in the brain of 5XFAD Alzheimer transgenic mouse model>, Application of C8H9NO3, the main research area is alzheimer disease brain amyloid beta.

Alzheimer disease (AD) is a neurodegenerative disorder characterized by the aberrant production and accumulation of amyloid-β (Aβ) peptides in the brain. Accumulated Aβ in soluble oligomer and insoluble plaque forms are considered to be a pathol. culprit and biomarker of the disorder. Here, we report a fluorescent universal Aβ-indicator YI-13, 5-(4-fluorobenzoyl)-7,8-dihydropyrrolo[1,2-b]isoquinolin-9(6H)-one, which detects Aβ monomers, dimers, and plaques. We synthesized a library of 26 fluorescence chems. with the indolizine core and screen them through a series of in vitro tests utilizing Aβ as a target and YI-13 was selected as the final imaging candidate. YI-13 was found to stain and visualize insoluble Aβ plaques in the brain tissue, of a transgenic mouse model with five familial AD mutations (5XFAD), by a histochem. approach and to label soluble Aβ oligomers within brain lysates of the mouse model under a fluorescence plate reader. Among oligomers aggregated from monomers and synthetic dimers from chem. conjugated monomers, YI-13 preferred the dimeric Aβ.

PLoS One published new progress about Alzheimer disease. 7126-50-3 belongs to class esters-buliding-blocks, and the molecular formula is C8H9NO3, Application of C8H9NO3.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Chen, Yuan; Fu, Lulu; Sun, Baobao; Qian, Cheng; Wang, Ruibing; Jiang, Juli; Lin, Chen; Ma, Jing; Wang, Leyong published the artcile< Competitive Selection of Conformation Chirality of Water-Soluble Pillar[5]arene Induced by Amino Acid Derivatives>, Category: esters-buliding-blocks, the main research area is amino acid ethyl ester hydrochloride induced conformation chirality pillararene.

The competitive conformation chirality of dynamically racemic water-soluble pillar[5]arene WP5 can be induced by 19 different L-amino acid Et ester hydrochlorides. Among them, L-Arg-OEt and 18 other L-amino acid Et ester hydrochlorides can induce the opposite-handedness conformation of WP5. This was ascribed to the different binding models with a side-chain moiety or Et ester moiety of amino acids toward the cavity of WP5.

Organic Letters published new progress about Amino acid esters Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation) (hydrochlorides). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yao, Tu; Xu, Pengfei; Xu, Xin published the artcile< Scandium complexes containing β-diketiminato ligands with pendant phosphanyl groups: competition between Sc/γ-C [4 + 2] cycloaddition and Sc/P frustrated Lewis pair reactions>, Formula: C11H13NS, the main research area is scandium diketiminato pendant phosphine cycloaddition frustrated Lewis pair reactivity; crystal structure scandium diketiminate phosphine chelate enolate preparation; polymerization catalyst frustrated Lewis pair scandium phosphino diketiminate.

Three cationic Sc aryloxide complexes, i.e., [LScOAr]+[B(C6F5)4]- (Ar = 2,6-tBu2C6H3; L = CH3C(2,6-iPr2C6H3N)C(R)CMe(N(CH2)nCH2PPh2); 6a: n = 1, R = H; 6b: n = 1, R = CH3; 6c: n = 2, R = C6H5CH2), were prepared by a three-step synthetic route. The reactivities of tridentate NNP ligand supported Sc complexes 6 toward various unsaturated substrates were studied. Treatment of 6a with nonconjugated small mols. such as Ph isocyanates, Ph isothiocyanate, and benzaldehyde gave Sc/γ-C [4 + 2] cycloaddition products because of nucleophilic reactivity at the β-diketiminato γ-C, with retention of Sc···P interactions. Analogous Sc/γ-C [4 + 2] cycloaddition reactions occurred for complex 6b with Ph isocyanate and Ph isothiocyanate. Complex 6c, with a bulky benzyl substituent at the γ position of the β-diketiminato ligand, showed typical Sc/P frustrated Lewis pair (FLP) reactivity toward Ph isocyanate to give a 1,2-addition product. Complex 6c was efficient in the polymerization of γ-methyl-α-methylene-γ-butyrolactone (MMBL). The corresponding initiating species, which was formed by Sc/P FLP-type 1,4-addition, was isolated.

Dalton Transactions published new progress about Crystal structure. 19241-24-8 belongs to class esters-buliding-blocks, and the molecular formula is C11H13NS, Formula: C11H13NS.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Tenti, Giammarco; Cores, Angel; Ramos, Maria Teresa; Menendez, J. Carlos published the artcile< (E)-3-((2-fluorophenyl)(hydroxy)methylene)imidazo[1,2-a]pyridin-2(3H)-one>, Recommanded Product: Ethyl 3-oxo-3-phenylpropanoate, the main research area is imidazopyridinone methylene hydroxy fluorophenyl preparation diastereoselective; pyridyl bromine ketoamide domino bromination cyclization tautomerism.

Treatment of a 3-(2-fluorophenyl)-3-oxo-N-(pyridin-2-yl)propanamide precursor with bromine afforded the first example of the (E)-3-((2-fluorophenyl)(hydroxy)methylene)imidazo[1,2-a]pyridin-2(3H)-one framework. This transformation proceeded through a domino process comprising an initial bromination, cyclization via an intramol. SN reaction, and a final keto-enol tautomerism, and allows generation of the fused heterocyclic system and installation of the acyl substituent in a single operation.

Molbank published new progress about Bromination. 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, Recommanded Product: Ethyl 3-oxo-3-phenylpropanoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Listowsky, Irving; Englard, Sasha; Avigad, Gad published the artcile< Conformational aspects of acidic sugars. Circular dichroism studies>, Synthetic Route of 617-55-0, the main research area is CD conformation sugar acid.

CD spectra were determined for 9 (S)-α-hydroxy acids, 7 (R)-aliphatic acids, and 6 monosaccharide acids. A rule was formulated which relates the sign of the observed ellipticity bands to the orientations of substituents relative to the carboxyl chromophore and explains the observed CD properties of the uronic and muramic acids.

Transactions of the New York Academy of Sciences published new progress about Circular dichroism. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Synthetic Route of 617-55-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics