Month: December 2022

Homerin, Germain published the artcilePyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease, Synthetic Route of 617-52-7, the publication is Journal of Medicinal Chemistry (2020), 63(5), 2074-2094, database is CAplus and MEDLINE.

This report deals with the design, the synthesis, and the pharmacol. evaluation of pyroglutamide-based P2X7 antagonists. A dozen were shown to possess improved properties, among which inhibition of YO-PRO-1/TO-PRO-3 uptake and IL1β release upon BzATP activation of the receptor and dampening signs of DSS-induced colitis on mice, in comparison with reference antagonist GSK1370319A. Docking study and biol. evaluation of synthesized compounds has highlighted new SAR, and low toxicity profiles of pyroglutamides herein described are clues for the finding of a usable h-P2X7 antagonist drug. Such a drug would raise the hope for a cure to many P2X7-dependent pathologies, including inflammatory, neurol., and immune diseases.

Journal of Medicinal Chemistry published new progress about 617-52-7. 617-52-7 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Aliphatic hydrocarbon chain,Ester, name is Dimethyl itaconate, and the molecular formula is C7H10O4, Synthetic Route of 617-52-7.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Yoshimura, Akira published the artcileHypervalent Iodine(III) Reagent Mediated Regioselective Cycloaddition of Aldoximes with Enaminones, SDS of cas: 924-99-2, the publication is European Journal of Organic Chemistry (2019), 2019(39), 6682-6689, database is CAplus.

An efficient oxidative cycloaddition of enaminones with nitrile oxides generated in situ from resp. aldoximes using hypervalent iodine reagent was developed for the synthesis of 3,4-disubstituted isoxazoles I [R = n-Pr, Ph, 1-naphthyl, etc.; R¹ = H, Me, Ph, etc.; R² = H, Me]. Reactions of various aldoximes with enaminones in the presence of [hydroxy(tosyloxy)iodo]benzene involved the regioselective cycloaddition reaction resulting in the formation of products I in moderate to good yields. Structures of several isoxazole products were confirmed by a single X-ray crystallog.

European Journal of Organic Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C8H5IO, SDS of cas: 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Brink, Madri published the artcileReduction of dietary crude protein and feed form: Impact on broiler litter quality, ammonia concentrations, excreta composition, performance, welfare, and meat quality, Safety of Propyl 3,4,5-trihydroxybenzoate, the publication is Animal Nutrition (2022), 291-303, database is CAplus and MEDLINE.

Nitrogen (N) excreted by poultry is converted to ammonia (NH3), presenting an environmental risk and a health risk to the farmer and animals. A study was performed to investigate the effect of reduced CP and feed form on broiler performance and welfare, meat and litter quality, N utilization, and NH3 concentrations at litter level. A total of 2,232 Ross 308 male broilers was divided into 6 treatments and 6 replicates, which was fed diets in both pellet and mash forms with different CP levels of 205.0 g/kg (H, high), 187.5 g/kg (M, intermediate) and 175.0 g/kg (L, low) in the grower phase and 195.0 g/kg (H), 180.0 g/kg (M) and 165.6 g/kg (L) in the finisher phase. Individual amino acids (AA) were supplemented to maintain digestible AA-to-digestible lysine ratios. Decreasing dietary CP content to 187.5 g/kg in the grower phase and 180.0 g/kg in the finisher phase reduced NH3 concentrations at litter level (P < 0.001), but a further reduction in dietary CP had no addnl. effect. Mash treatments had better litter qualities and lower incidences of foot and hock lesions than pellet treatments at d 38 (P < 0.001). In addition, treatments with reduced CP had lower incidence of foot lesions at d 38 (P < 0.001). Broilers fed pelleted diets had higher ADFI, ADG, and final BW, improved feed conversion ratio (FCR), and heavier carcasses (P < 0.001) than those fed mash diets over a production period of 39 d. Performance could not be maintained when birds were fed L CP pelleted diets. This study demonstrated that, with the supplementation of AA to meet requirements, the concentration of dietary CP can be reduced to 187.5 and 180.0 g/kg in the grower and finisher phases resp., without impairing broiler performance, meat yield and quality. Mash diets were favorable when considering the overall litter quality and welfare of the birds. However, they could not maintain the same broiler performance and slaughter yield as pelleted diets. Results from the present study may assist the poultry sector towards a socially acceptable low-emission farming system.

Animal Nutrition published new progress about 121-79-9. 121-79-9 belongs to esters-buliding-blocks, auxiliary class Natural product, name is Propyl 3,4,5-trihydroxybenzoate, and the molecular formula is C10H12O5, Safety of Propyl 3,4,5-trihydroxybenzoate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Kang, Suk Hoon published the artcilePhotoimaging through in-Situ Photopolymerization of Heterobifunctional Mesogenic Compounds in Liquid Crystalline State, Category: esters-buliding-blocks, the publication is Macromolecules (Washington, DC, United States) (2007), 40(23), 8349-8354, database is CAplus.

A series of heterobifunctional mesogenic biphenyl esters having two different polymerizable groups, i.e., acryl and diacetylene groups, were synthesized and their thermal behaviors and polymerization investigated. All compounds showed enantiotropic transitions. Under POM, highly birefringent focal-conic fan textures appeared on heating and cooling from the isotropic melt. Compounds 6-8 having a Bu spacer between a biphenyl and a diacetylene group exhibited LC phases even at room temperature The x-ray diffractograms of compounds 6-8 showed a set of reflections in the small-angle region. They consisted of more than three sharp diffraction peaks with d spacings in the ratio of 1:1/2:1/3, showing that the compounds had well-defined smectic A structures. For the photoimaging a mixture of 6 and a photoinitiator (2,2-dimethoxy-2-phenylacetophenone, 4 wt %) was cast on a glass plate and sheared with a cover glass at room temperature to result in an LC monodomain. The acryl group was then selectively polymerized by irradiation with low-intensity 365 nm UV light to yield a polymer film. Subsequent UV irradiation at 254 nm using a 100 W high-pressure mercury arc lamp through a photomask produced conjugated polyacetylene chains in the irradiated area. The polydiacetylene chains were fluorescent, and the patterned image was directly visualized by fluorescence microscopy.

Macromolecules (Washington, DC, United States) published new progress about 50670-76-3. 50670-76-3 belongs to esters-buliding-blocks, auxiliary class Benzene,Phenol,Ester, name is Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate, and the molecular formula is C15H14O3, Category: esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Ahmed, Sabbir published the artcileDesign, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES), Application In Synthesis of 50670-76-3, the publication is Bioorganic & Medicinal Chemistry Letters (2002), 12(10), 1343-1346, database is CAplus and MEDLINE.

4-(4-RC₆H₄)C₆H₄O₃SNH₂ [= H, CN, CO₂Me, CO₂Et, CO₂Pr, CO₂Bu] were preparedas novel inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than coumate, but weaker inhibitory activity than emate or the tricyclic derivative of coumate, namely 667-coumate. Furthermore, the compounds are observed to be irreversible inhibitors.

Bioorganic & Medicinal Chemistry Letters published new progress about 50670-76-3. 50670-76-3 belongs to esters-buliding-blocks, auxiliary class Benzene,Phenol,Ester, name is Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate, and the molecular formula is C15H14O3, Application In Synthesis of 50670-76-3.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Ahmed, Sabbir published the artcileDesign, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES), Recommanded Product: Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate, the publication is Journal of Steroid Biochemistry and Molecular Biology (2003), 82(4-5), 425-435, database is CAplus and MEDLINE.

We report the results of our study into a series of 4′-O-sulfamoyl-4-biphenyl based compounds as novel inhibitors of the enzyme estrone sulfatase (ES). From the results of the mol. modeling design process, it was suggested that these compounds would be able to mimic both the A and C rings of the steroid backbone, and thus possess inhibitory activity against ES. The results of the biochem. evaluation study show that these compounds are indeed good inhibitors, possessing greater inhibitory activity than COUMATE, but weaker inhibitory activity than EMATE or the tricyclic derivative of COUMATE, namely 667-COUMATE. Furthermore, the compounds are observed to be irreversible inhibitors.

Journal of Steroid Biochemistry and Molecular Biology published new progress about 50670-76-3. 50670-76-3 belongs to esters-buliding-blocks, auxiliary class Benzene,Phenol,Ester, name is Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate, and the molecular formula is C15H14O3, Recommanded Product: Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Hofmeister, Armin published the artcileSyntheses of Morpholine-Based Nucleotide Analogs for Hepatic siRNA Targeting and Stabilization, Category: esters-buliding-blocks, the publication is Journal of Medicinal Chemistry (2021), 64(10), 6838-6855, database is CAplus and MEDLINE.

A morpholine-based nucleotide analog was developed as a building block for hepatic siRNA targeting and stabilization. Attachment of an asialoglycoprotein-binding GalNAc ligand at the morpholine nitrogen was realized with different linkers. The obtained morpholino GalNAc scaffolds were coupled to the sense strand of a transthyretin-targeting siRNA and tested for their knockdown potency in vitro and in vivo. A clear structure-activity relationship was developed with regard to the linker type and length as well as the attachment site of the morpholino GalNAc moieties at the siRNA sense strand. Further, simple alkylation of the morpholine nitrogen led to a nucleotide analog, which increased siRNA stability, when used as a double 3′-overhang at the sense strand sequence. Combination of the best morpholino GalNAc building blocks as targeting nucleotides with an optimized stabilizing alkyl-substituted morpholine as 3′-overhangs resulted in siRNAs without any phosphorothioate stabilization in the sense strand and clearly improved the duration of action in vivo.

Journal of Medicinal Chemistry published new progress about 10378-06-0. 10378-06-0 belongs to esters-buliding-blocks, auxiliary class Other Aliphatic Heterocyclic,Chiral,Ester,Inhibitor,Inhibitor, name is (3aR,5R,6R,7R,7aR)-5-(Acetoxymethyl)-2-methyl-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]oxazole-6,7-diyl diacetate, and the molecular formula is C14H19NO8, Category: esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Jahjah, Mohamad published the artcileAsymmetric hydrogenation of aromatic ketones with new P-chirogenic monophosphine ligands, Product Details of C22H12F6O6S2, the publication is Tetrahedron: Asymmetry (2007), 18(10), 1224-1232, database is CAplus.

Novel P-chirogenic anisylphenyl-HMOP derivatives were synthesized from (R)-2,2′-bis(trifluoromethanesulfonyloxy)-1,1′-binaphthyl. Preliminary results concerning the asym. hydrogenation of acetophenone and 3,5-bis(trifluoromethyl)acetophenone with Ru(II)-HMOP complexes in combination with various diamines was also tackled. (R)-((R)-1,1′-binaphthalen-2-yl)(2-methoxyphenyl)(phenyl)phosphine, bis[(η⁶-benzene)dichlororuthenium], and 1,4-diaminobutane gave the best results with acetophenone, i.e. 61 %ee for 100 % conversion.

Tetrahedron: Asymmetry published new progress about 126613-06-7. 126613-06-7 belongs to esters-buliding-blocks, auxiliary class Chiral Diphenols, name is (R)-[1,1′-Binaphthalene]-2,2′-diyl bis(trifluoromethanesulfonate), and the molecular formula is C22H12F6O6S2, Product Details of C22H12F6O6S2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Alame, M. published the artcile2,2′-Bis-[bis(4-substituted-phenyl)phosphino]-1,1′-binaphthyl derivatives in Rh(I)-catalyzed hydrogenation of acetamidoacrylic acid derivatives: Electronic effects, Product Details of C22H12F6O6S2, the publication is Journal of Molecular Catalysis A: Chemical (2007), 271(1-2), 18-24, database is CAplus.

Electronic effects of electron-donating and electron-withdrawing substituents at the para position of the Ph moieties of BINAP ligands were studied towards asym. hydrogenation of α-(acylamino)acrylic acids. Enantiomeric excesses varied as a linear relationship towards Hammett coefficients σ_p of electron-donating groups between 0 and -0.63.

Journal of Molecular Catalysis A: Chemical published new progress about 126613-06-7. 126613-06-7 belongs to esters-buliding-blocks, auxiliary class Chiral Diphenols, name is (R)-[1,1′-Binaphthalene]-2,2′-diyl bis(trifluoromethanesulfonate), and the molecular formula is C22H12F6O6S2, Product Details of C22H12F6O6S2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

van Dort, Hans M. published the artcileNarcissus trevithian and Narcissus geranium: Analysis and synthesis of compounds, Name: 3-Methylbut-2-en-1-yl benzoate, the publication is Journal of Agricultural and Food Chemistry (1993), 41(11), 2063-75, database is CAplus.

The essential oils of two Narcissus varieties, N. trevithian and N.geranium, obtained by extraction of flowers followed by high vacuum distillation of the absolute, were analyzed by GC/MS. After separation in fractions, unknown compounds were isolated by preparative GLC and their structures established by NMR/IR spectroscopy. The synthesis of a number of new compounds, found for the first time in narcissus oil, is described. The two narcissus species are compared with respect to their main components and odor quality. All compounds found so far in narcissus varieties are listed.

Journal of Agricultural and Food Chemistry published new progress about 5205-11-8. 5205-11-8 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Benzene,Ester, name is 3-Methylbut-2-en-1-yl benzoate, and the molecular formula is C6H16OSi, Name: 3-Methylbut-2-en-1-yl benzoate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics