Esters-buliding-blocks

Gulyas, Henrik published the artcileHighly active, chemo- and enantioselective Pt-SPO catalytic systems for the synthesis of aromatic carboxamides, Related Products of esters-buliding-blocks, the publication is Catalysis Science & Technology (2015), 5(7), 3822-3828, database is CAplus.

Platinum complexes modified with a chiral non-racemizing SPO pre-ligand have been applied in the hydration of aromatic nitriles. [Pt(1)₃Cl]Cl formed readily from Pt(COD)Cl₂. A chiral secondary phosphine oxide complex showed moderate activity in the hydration of para- and meta-substituted benzonitriles, but failed in converting the ortho-substituted derivatives The hydride complex PtH(PR₂OH)(PR₂O-H···OR₂P) (PR₂OH = 1) formed from Pt(PPh₃)₄ and 1, and the cationic complex derived from [Pt(1)₃Cl]Cl by a direct chloride abstraction with AgNO₃ were proven to be considerably more active, allowing us to extend the scope to the hydration of ortho-substituted aromatic nitriles, including axially chiral [1,1′-binaphthalene]-2,2′-dicarbonitrile. In the hydration of a racemic dinitrile, successful kinetic resolution has been achieved. The catalysts derived from a non-racemizing ligand are the first chiral transition metal-SPO complexes that provide kinetic resolution in the hydration of a racemic chiral nitrile. The synthesis of the target compounds was achieved using (11bR)-4,5-dihydro-3H-Dinaphtho[2,1-c:1′,2′-e]phosphepin 4-oxide as a chiral ligand and dichloro[(1,2,5,6-η)-1,5-cyclooctadiene]platinum or tetrakis(triphenylphosphine)platinum as catalyst. Starting materials included benzonitrile derivatives, naphthalenecarbonitrile, benzeneacetonitrile., [1,1′-binaphthalene]-2,2′-dicarbonitrile.

Catalysis Science & Technology 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, Related Products of esters-buliding-blocks.

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

Aprile, Silvio published the artcile1,2,4-Oxadiazole-Bearing Pyrazoles as Metabolically Stable Modulators of Store-Operated Calcium Entry, Computed Properties of 1877-71-0, the publication is ACS Medicinal Chemistry Letters (2021), 12(4), 640-646, database is CAplus and MEDLINE.

Store-operated calcium entry (SOCE) is a pivotal mechanism in calcium homeostasis, and, despite still being under investigation, its dysregulation is known to be associated with severe human disorders. SOCE modulators are therefore needed both as chem. probes and as therapeutic agents. While many small mols. have been described so far, their poor properties in terms of drug-likeness have limited their translation into the clin. practice. In this work, we describe the bioisosteric replacement of the ester moiety in pyrazole derivatives with a 1,2,4-oxadiazole ring as a means to afford a class of modulators with high metabolic stability. Moreover, among our derivatives, a compound able to increase the calcium entry was identified, further enriching the library of available SOCE activators.

ACS Medicinal Chemistry Letters published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Computed Properties of 1877-71-0.

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

Duncan, Kenneth W. published the artcileStructure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666, Computed Properties of 115314-17-5, the publication is ACS Medicinal Chemistry Letters (2016), 7(2), 162-166, database is CAplus and MEDLINE.

The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound I (EPZ015666, GSK3235025) to probe the underlying pharmacol. of this key enzyme. Herein, the authors report the design and optimization strategies employed on an initial hit compound with poor in vitro clearance to yield in vivo tool compound I and an addnl. potent in vitro tool mol. II (GSK3203591).

ACS Medicinal Chemistry Letters published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Computed Properties of 115314-17-5.

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

Reina, Jose J. published the artcileGlycosyl Aldehydes: New Scaffolds for the Synthesis of Neoglycoconjugates via Bioorthogonal Oxime Bond Formation, Formula: C14H19NO8, the publication is Synthesis (2018), 50(4), 831-845, database is CAplus.

The straightforward preparation of glycosyl neoconjugates by oxime (or hydrazone) bond formation represents a key bioorthogonal tool in chem. biol. However, when this strategy is employed by reacting the reducing end of the glycan moiety, the configuration and the stereochem. information is lost due to partial (or complete) opening of the glycan cyclic hemiacetal and the formation of the corresponding opened tautomers. We have completed the synthesis of a library of glycosyl aldehydes to be used as scaffold for the synthesis of neoglycoconjugates via oxime bond formation. These glycosyl aldehydes constitute a simple and accessible alternative to avoid loss of chiral information when conjugating, by oxime (or hydrazone) bonds, the aldehyde functionality present at the reducing end of natural carbohydrates.

Synthesis 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, Formula: C14H19NO8.

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

Benini, Celine published the artcileVariations in the essential oils from ylang-ylang (Cananga odorata [Lam.] Hook f. & Thomson forma genuina) in the Western Indian Ocean islands, Product Details of C12H14O2, the publication is Flavour and Fragrance Journal (2012), 27(5), 356-366, database is CAplus.

Ylang-ylang essential oil is an important raw material for the fragrance industry. Despite its economic importance, to the best of our knowledge, no study has yet been undertaken to assess the chem. polymorphism of the different production areas. This underestimated variability is an interesting source of raw material for perfumers. That is why the variation in the chem. composition of four fractions of the essential oils extracted from Cananga odorata, grown in four locations Grande Comore, Mayotte, Nossi Be and Ambanja, was studied. A total of 119 compounds, representing 85.7-96.4% of the total essential oil composition, were identified using gas chromatog.-mass spectrometry and quantified by gas chromatog. with a flame ionization detector. Thirty-two compounds previously unreported in ylang-ylang essential oil were identified. The distinction between the Comoros and Madagascar groups was made on the basis of the chem. classes. It was possible to significantly distinguish the Grande Comore and Mayotte essential oil samples, as well as the Ambanja and Nossi Be essential oil samples, on the basis of their main compounds The aromatic compounds profile for the origin of each essential oil fraction was established. Regression trees were built, allowing the provenance of the essential oils prepared at the laboratory level to be easily differentiated on the basis of a limited number of major compounds Copyright © 2012 John Wiley & Sons, Ltd.

Flavour and Fragrance Journal 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 C12H14O2, Product Details of C12H14O2.

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

Pinto, Barbara Fernandes published the artcileInhalation of dimethyl fumarate-encapsulated solid lipid nanoparticles attenuate clinical signs of experimental autoimmune encephalomyelitis and pulmonary inflammatory dysfunction in mice, Quality Control of 624-49-7, the publication is Clinical Science (2022), 136(1), 81-101, database is CAplus and MEDLINE.

The FDA-approved Di-Me Fumarate (DMF) as an oral drug for Multiple Sclerosis (MS) treatment based on its immunomodulatory activities. However, it also caused severe adverse effects mainly related to the gastrointestinal system. Investigated the potential effects of solid lipid nanoparticles (SLNs) containing DMF, administered by inhalation on the clin. signs, central nervous system (CNS) inflammatory response, and lung function changes in mice with exptl. autoimmune encephalomyelitis (EAE). EAE was induced using MOG35-55 peptide in female C57BL/6J mice and the mice were treated via inhalation with DMF-encapsulated SLN (CTRL/SLN/DMF and EAE/SLN/DMF), empty SLN (CTRL/SLN and EAE/SLN), or saline solution (CTRL/saline and EAE/saline), every 72 h during 21 days. After 21 days post-induction, EAE mice treated with DMF-loaded SLN, when compared with EAE/saline and EAE/SLN, showed decreased clin. score and weight loss, reduction in brain and spinal cord injury and inflammation, also related to the increased influx of Foxp3+ cells into the spinal cord and lung tissues. Moreover, our data revealed that EAE mice showed signs of respiratory disease, marked by increased vascular permeability, leukocyte influx, production of TNF-a and IL-17, perivascular and peribronchial inflammation, with pulmonary mech. dysfunction associated with loss of respiratory volumes and elasticity, which DMF-encapsulated reverted in SLN nebulization. Our study suggests that inhalation of DMF-encapsulated SLN is an effective therapeutic protocol that reduces not only the CNS inflammatory process and disability progression, characteristic of EAE disease, but also protects mice from lung inflammation and pulmonary dysfunction.

Clinical Science published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Quality Control of 624-49-7.

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

Tran, Huy published the artcileDivergent and Modular Synthesis of Terpenoid Scaffolds via a Au^I Catalyzed One-Pot Cascade, SDS of cas: 624-49-7, the publication is Angewandte Chemie, International Edition (2022), 61(1), e202110575, database is CAplus and MEDLINE.

A one-pot cascade sequence to generate synthetically challenging polycyclic scaffolds is reported utilizing a novel Lewis acid gold catalyst for the key cyclization step, enabling the divergent synthesis of both 6,6,5-tricyclic and 6,6,6,5-tetracyclic cores through both ligand and reaction condition control. We have combined the intrinsic complexity and stereoselectivity of cycloadditions with the electronic and steric properties of gold complexes to selectively generate complex polycyclic scaffolds in a single operation.

Angewandte Chemie, International Edition published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C5H9IO2, SDS of cas: 624-49-7.

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

Sobolevsky, Tim G. published the artcileSimultaneous determination of fatty, dicarboxylic and amino acids based on derivatization with isobutyl chloroformate followed by gas chromatography-positive ion chemical ionization mass spectrometry, Computed Properties of 110-34-9, the publication is Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences (2004), 800(1-2), 101-107, database is CAplus and MEDLINE.

Gas chromatog.-mass spectrometry (GC-MS) with pos. ion chem. ionization (PICI) using isobutane as reagent gas was applied for anal. of isobutoxycarbonyl/isobutyl derivatives of 13 fatty, 6 dicarboxylic and 13 amino acids in a single run. For all investigated compounds (except several amino acids) the quasimol. ions [MH]⁺ were registered. Asparagine underwent fragmentation via decarboxylation followed by elimination of OC₄H₉ ([M-117]⁺), whereas serine and tyrosine produced the cluster ions [M + C₄H₉OCO]⁺. Estimated detection limits were 6-250 pg in the total ion current (TIC) mode and 3-10 times lower using the selected-ion monitoring (SIM) mode.

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences published new progress about 110-34-9. 110-34-9 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester, name is Isobutyl palmitate, and the molecular formula is C4Br2N2O4S, Computed Properties of 110-34-9.

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

Pechenov, Sergei published the artcileDevelopment of an orally delivered GLP-1 receptor agonist through peptide engineering and drug delivery to treat chronic disease, Safety of Propyl 3,4,5-trihydroxybenzoate, the publication is Scientific Reports (2021), 11(1), 22521, database is CAplus and MEDLINE.

Peptide therapeutics are increasingly used in the treatment of disease, but their administration by injection reduces patient compliance and convenience, especially for chronic diseases. Thus, oral administration of a peptide therapeutic represents a significant advance in medicine, but is challenged by gastrointestinal instability and ineffective uptake into the circulation. Here, we have used glucagon-like peptide-1 (GLP-1) as a model peptide therapeutic for treating obesity-linked type 2 diabetes, a common chronic disease. We describe a comprehensive multidisciplinary approach leading to the development of MEDI7219, a GLP-1 receptor agonist (GLP-1RA) specifically engineered for oral delivery. Sites of protease/peptidase vulnerabilities in GLP-1 were removed by amino acid substitution and the peptide backbone was bis-lipidated to promote MEDI7219 reversible plasma protein binding without affecting potency. A combination of sodium chenodeoxycholate and Pr gallate was used to enhance bioavailability of MEDI7219 at the site of maximal gastrointestinal absorption, targeted by enteric-coated tablets. This synergistic approach resulted in MEDI7219 bioavailability of ∼ 6% in dogs receiving oral tablets. In a dog model of obesity and insulin resistance, MEDI7219 oral tablets significantly decreased food intake, body weight and glucose excursions, validating the approach. This novel approach to the development of MEDI7219 provides a template for the development of other oral peptide therapeutics.

Scientific Reports 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

Parker, Belinda S. published the artcileFormation of mitoxantrone adducts in human tumor cells: potentiation by AN-9 and DNA methylation, Application of (Pivaloyloxy)methyl butyrate, the publication is Oncology Research (2004), 14(6), 279-290, database is CAplus and MEDLINE.

The ability of mitoxantrone to form DNA adducts was investigated in a series of human tumor cell lines consisting of human cervical cancer (HeLa), human breast cancer (MCF-7), and human neuroblastoma (IMR-32) cells. The mitoxantrone-resistant human promyelocytic leukemia cell line HL60/MX2 was also compared to the parental cell line HL60 in terms of adduct formation in cellular DNA, RNA, and protein. DNA adduct formation detected using [¹⁴C]mitoxantrone as a single agent occurred at very low levels but addition of the formaldehyde-releasing prodrug AN-9 (pivaloyloxymethyl butyrate) increased adduct formation considerably in all cell lines tested. Adduct formation increased when increasing ratios of AN-9 were used, and were observed at maximal levels when AN-9 addition was 4 h after the addition of mitoxantrone. However, low levels of adducts were observed when AN-9 addition was 16 h prior to mitoxantrone. The ability of [¹⁴C]mitoxantrone to form adducts with DNA, RNA, and protein was assessed in HL60 cells, and DNA was found to be the major substrate for adduct formation. RNA was also shown to be a good substrate while protein adduct levels were consistently very low. In mitoxantrone-resistant HL60/MX2 cells, DNA adduct levels were approx. fourfold lower. To establish the influence of DNA methylation on the ability of mitoxantrone to form adducts in cells, decitabine was used to reduce DNA methylation levels in cells prior to mitoxantrone treatment. This was clearly shown to influence adduct formation, with increasing decitabine levels leading to a decrease in the level of adducts observed in both IMR-32 and MCF-7 cell lines. Collectively, these results suggest that two major factors that influence the extent of mitoxantrone adduct formation in cells are the availability of formaldehyde and the extent of genomic DNA methylation.

Oncology Research published new progress about 122110-53-6. 122110-53-6 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ester,Inhibitor, name is (Pivaloyloxy)methyl butyrate, and the molecular formula is C10H18O4, Application of (Pivaloyloxy)methyl butyrate.

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