Month: December 2022

Skorenski, Marcin published the artcilePhosphonate inhibitors of West Nile virus NS2B/NS3 protease, Application of 4,4-Diethoxybutan-1-amine, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2019), 34(1), 8-14, database is CAplus and MEDLINE.

West Nile virus (WNV) is a member of the flavivirus genus belonging to the Flaviviridae family. The viral serine protease NS2B/NS3 has been considered an attractive target for the development of anti-WNV agents. Although several NS2B/NS3 protease inhibitors have been described so far, most of them are reversible inhibitors. Herein, we present a series of α-aminoalkylphosphonate di-Ph esters and their peptidyl derivatives as potent inhibitors of the NS2B/NS3 protease. The most potent inhibitor identified was Cbz-Lys-Arg-(4-GuPhe)^P(OPh)₂ displaying K_i and k₂/K_i values of 0.4 μM and 28 265 M^-1s^-1, resp., with no significant inhibition of trypsin, cathepsin G, and HAT protease.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 6346-09-4. 6346-09-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Ether, name is 4,4-Diethoxybutan-1-amine, and the molecular formula is C15H14O3, Application of 4,4-Diethoxybutan-1-amine.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Marinov, B published the artcile[Some possibilities for application of “Pfizer” medicines–Prostin 15m, Prostin E2, Prepidil gel, Dostinex, Synarel–in the obstetrician practice]., Recommanded Product: 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, the publication is Akusherstvo i ginekologiia (2007), 57-60, database is MEDLINE.

The authors make a clinical and pharmacological overview of the possibilities of application in the obstetrician practice of part of the medicines of the company Pfiser. Some of these medicines have no analogue in Bulgaria–i.e. Prostin 15M. The authors outline the advantages of the Pfiser medicines in comparison with other medicines with similar action.

Akusherstvo i ginekologiia published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C25H47NO8, Recommanded Product: 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Kinosita, Yoshiaki published the artcileMotile ghosts of the halophilic archaeon, Haloferax volcanii, Application of Triisopropanolamine, the publication is Proceedings of the National Academy of Sciences of the United States of America (2020), 117(43), 26766-26772, database is CAplus and MEDLINE.

Archaea swim using the archaellum (archaeal flagellum), a reversible rotary motor consisting of a torque-generating motor and a helical filament, which acts as a propeller. Unlike the bacterial flagellar motor (BFM), ATP (adenosine-5a²-triphosphate) hydrolysis probably drives both motor rotation and filamentous assembly in the archaellum. However, direct evidence is still lacking due to the lack of a versatile model system. Here, we present a membrane-permeabilized ghost system that enables the manipulation of intracellular contents, analogous to the triton model in eukaryotic flagella and gliding Mycoplasma. We observed high nucleotide selectivity for ATP driving motor rotation, neg. cooperativity in ATP hydrolysis, and the energetic requirement for at least 12 ATP mols. to be hydrolyzed per revolution of the motor. The response regulator CheY increased motor switching from counterclockwise (CCW) to clockwise (CW) rotation. Finally, we constructed the torque-speed curve at various [ATP]s and discuss rotary models in which the archaellum has characteristics of both the BFM and F1-ATPase. Because archaea share similar cell division and chemotaxis machinery with other domains of life, our ghost model will be an important tool for the exploration of the universality, diversity, and evolution of biomol. machinery.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 122-20-3. 122-20-3 belongs to alcohols-buliding-blocks, auxiliary class Organic Pigment, name is Triisopropanolamine, and the molecular formula is C9H21NO3, Application of Triisopropanolamine.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Ferreira Azevedo, L. published the artcileThe alternative analog plasticizer BPS displays similar phenotypic and metabolomic responses to BPA in HepG2 and INS-1E cells, COA of Formula: C12H10O4S, the publication is Food and Chemical Toxicology (2022), 167(Suppl._1), 113266, database is CAplus and MEDLINE.

Bisphenols A (BPA) and S (BPS) are endocrine-disrupting chems. that affect energy metabolism, leading to impairment of glucose and lipid homeostasis. We aimed at identifying metabolic pathways regulated by both compounds in human liver cells and rat pancreatic β-cells that could impair energy homeostasis regulation. We assessed the effects on growth, proliferation, and viability of hepatocarcinoma (HepG2) and insulinoma (INS-1E) cells exposed to either BPA or BPS in a full range concentration between 0.001 and 100μM. Both the dose and duration of exposure caused a differential response on growth and viability of both cells. Effects were more pronounced on HepG2, as these cells exhibited non-linear dose-responses following exposure to xenobiotics. For INS-1E, effect was observed only at the highest concentration In addition, we profiled their intracellular state by untargeted metabolomics at 24, 48, and 72 h of exposure. This anal. revealed time- and dose-dependently mol. changes for HepG2 and INS-1E that were similar between BPA and BPS. Both increased levels of inflammatory mediators, such as metabolites pertaining to linolenic and linoleic acid metabolic pathway. In summary, this study shows that BPS also disrupts mol. functions in cells that regulate energy homeostasis, displaying similar but less pronounced responses than BPA.

Food and Chemical Toxicology published new progress about 80-09-1. 80-09-1 belongs to alcohols-buliding-blocks, auxiliary class Ploymers, name is 4,4′-Sulfonyldiphenol, and the molecular formula is C12H10O4S, COA of Formula: C12H10O4S.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Olechowska, Karolina published the artcileThe effect of selected bisphenols on model erythrocyte membranes of different cholesterol content, Category: alcohols-buliding-blocks, the publication is Chemistry and Physics of Lipids (2022), 105224, database is CAplus and MEDLINE.

Bisphenols belong to the group of environmental pollutants with proven harmful impact on human red blood cells. However, the exact effect of these substances may vary depending on the lipid composition of the cell membrane, since this structure is the first barrier between the cell interior and the external environment. The aim of this work was to analyze the influence of bisphenol A (BPA), bisphenol S (BPS) and their 1:1 mixture on model human erythrocyte membranes, composed of sphingomyelin (SM), phospatidylcholine (PC) and cholesterol (Chol). Due to the postulated correlation between the content of cholesterol in biomembranes and the toxic effect of bisphenols the model systems of different sterol concentrations (10, 20 and 40 mol% of Chol) were used in the studies. In the experiments, Langmuir monolayer technique accompanied with Brewster Angle Microscopy were applied and liposome properties were investigated. The obtained findings reveal that, in the investigated range of the sterol content, the effect of BPA, namely the changes of the organization and stability of model membranes and weakening of the attractive lipid-lipid interactions, is strongly dependent on the concentration of Chol in the system. The higher the sterol content, the stronger the BPA-induced alterations in membrane properties. However taking into account the results reported previously for the system containing 33.3% of cholesterol, it seems that the relationship between the effect of BPA and the amount of Chol is not linear for higher sterol concentrations In contrast, BPS shows a much weaker influence on model erythrocyte membranes and does not act selectively on the systems studied. The effect of a mixture of BPA and BPS is intermediate between that of BPA and BPS used sep., however, the observed effects appear to be determined only by the presence of BPA in the system. Thus, the concentration of cholesterol in human erythrocyte membranes, which depends on factors such as age or health status, may play a key role in the toxic effects of BPA but not BPS.

Chemistry and Physics of Lipids published new progress about 80-09-1. 80-09-1 belongs to alcohols-buliding-blocks, auxiliary class Ploymers, name is 4,4′-Sulfonyldiphenol, and the molecular formula is C12H10O4S, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Derrien, Daniele published the artcileMuramyl dipeptide bound to poly-L-lysine substituted with mannose and gluconoyl residues as macrophage activators, SDS of cas: 96345-79-8, the publication is Glycoconjugate Journal (1989), 6(2), 241-55, database is CAplus and MEDLINE.

Poly(L-lysine) modified with mannose derivatives, the residual cationic charges of which being neutralized by N-acylation, were synthesized and used as carriers of a macrophage activator (N-acetylmuramyl dipeptide, MDP). The effect of the acylating agent on the targeting efficiency was investigated: a hydrosolubilizing group such as a gluconoyl moiety led to very efficient carrier conjugates, while an acetyl group did not. The effect of sugar and acyl content of the polymers was assessed using these compounds as inhibitors of red blood cell agglutination by Con A. The binding and specific endocytosis of poly(L-lysine) substituted with several mannose derivatives and gluconoyl residues (GlcA_x-, Man_y-PLK) were determined by a quant. flow cytometry anal. MDP bound to these conjugates was much more efficient in vitro than free MDP in macrophage cytostasis assays.

Glycoconjugate Journal published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C13H15NO6S, SDS of cas: 96345-79-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Yuan, Yuping published the artcileEnergy level tuning of polythiophene derivative by click chemistry-type postfunctionalization of side-chain alkynes, Safety of 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, the publication is Journal of Polymer Science, Part A: Polymer Chemistry (2011), 49(1), 225-233, database is CAplus.

A polythiophene derivative substituted with electron-rich alkynes as a side chain was synthesized using the Suzuki polycondensation reaction. The electron-rich alkynes underwent the “click chem.”-type quant. addition reaction with strong acceptor mols., such as tetracyanoethylene (TCNE) and 7,7,8,8-tetracyanoquinodimethane (TCNQ), resulting in the formation of donor-acceptor chromophores. All polymers showed excellent solubilities in the common organic solvents as well as good thermal stabilities with their 5% decomposition temperatures exceeding 230 °C. The TCNE-/TCNQ-adducted polymers displayed well-defined charge-transfer (CT) bands in the low energy region. The CT energy of the TCNE-adducted polymer was 2.56 eV (484 nm), which was much greater than that of the TCNQ-adducted polymer [1.65 eV (750 nm)]. This result was supported by the electrochem. measurements. The electrochem. band gaps of the TCNE-adducted polymers were much greater than those of the corresponding TCNQ-adducted polymers. Furthermore, the HOMO and LUMO energy levels, determined from the first oxidation and first reduction peak potentials, resp., decreased with the increasing acceptor addition amount All these results suggested that the energy levels of the polythiophene derivative can be tuned by varying the species and amount of the acceptor mols. using this postfunctionalization method. © 2010 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2010.

Journal of Polymer Science, Part A: Polymer Chemistry published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C12H14S, Safety of 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Daldrup, T. published the artcileA screening test for pharmaceuticals, drugs and insecticides with reversed-phase liquid chromatography – retention data of 560 compounds, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Chromatography Newsletter (1982), 10(1), 1-7, database is CAplus.

High-performance reversed-phase liquid chromatog. retention data are given. The relative retention times were calculated as the ratio of retention times of compound and reference compound 5-(p-methylphenyl)-5-phenylhydantoin. The UV detector wavelength was 220 nm, where most of the compounds gave a good response. The sensitivity of the method for each compound is rated from very good to bad. Two solvent programs and a prepacked column C-18 SIL-X-10 were used for the anal.

Chromatography Newsletter published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bertrand, Guillaume H. V. published the artcileThiophene-based covalent organic frameworks, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, the publication is Proceedings of the National Academy of Sciences of the United States of America (2013), 110(13), 4923-4928, S4923/1-S4923/20, database is CAplus and MEDLINE.

We report the synthesis and characterization of covalent organic frameworks (COFs) incorporating thiophene-based building blocks. We show that these are amenable to reticular synthesis, and that bent ditopic monomers, such as 2,5-thiophenediboronic acid, are defect-prone building blocks that are susceptible to synthetic variations during COF synthesis. The synthesis and characterization of an unusual charge transfer complex between thieno[3,2-b]thiophene-2,5-diboronic acid and tetracyanoquinodimethane enabled by the unique COF architecture is also presented. Together, these results delineate important synthetic advances toward the implementation of COFs in electronic devices.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Wei, Piao-piao published the artcileAnalysis of Metabolites from Direct Fermentation of D-Glucose to 2-Keto-L-Gulonic Acid by HPLC, Application of (3S,4R,5S)-3,4,5,6-Tetrahydroxy-2-oxohexanoic acid, the publication is Guocheng Gongcheng Xuebao (2013), 13(4), 675-680, database is CAplus.

An HPLC-based method for quant. determination of the 4 metabolites of gluconic acid (GlcA), 2-keto-D-gluconic acid (2-KDG), 2,5-diketo-D-gluconic acid (2,5-DKG) and 2-keto-L-gulonic acid (2-KLG) from direct fermentation of D-glucose to 2-KLG by using HPLC was established. The optimum separation of the 4 substances could be achieved under the conditions of using Aminex HPX-87H column (size 300 mm x7.8 mm) with the temperature of 30 °C, sulfuric acid (50 mmol/L) as mobile phase at the flow rate of 0.2 mL/min, RID-10A detector, and malonic acid as internal standard The anal. results show that the method has average anal. deviation of 1.53%, 0.89% and 1.84% on 2-KDG 2,5-DKG and 2-KLG, resp.

Guocheng Gongcheng Xuebao published new progress about 526-98-7. 526-98-7 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Other Sugar Units, name is (3S,4R,5S)-3,4,5,6-Tetrahydroxy-2-oxohexanoic acid, and the molecular formula is C20H19NO4, Application of (3S,4R,5S)-3,4,5,6-Tetrahydroxy-2-oxohexanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts