Month: December 2022

Xie, Wen-Bin published the artcileBis(¦Ì-oxo)-Dititanium(IV)-Chiral Binaphthyldisulfonate Complexes for Highly Enantioselective Intramolecular Hydroalkoxylation of Nonactivated Alkenes, Synthetic Route of 2051-95-8, the publication is ACS Catalysis (2021), 11(10), 6270-6275, database is CAplus.

A series of chiral 1,1′-binaphthyl-2,2′-disulfonic acids was designed, synthesized, and applied in a highly enantioselective Ti-catalyzed intramol. hydroalkoxylation of nonactivated alkenes. The catalyst is probably a complex between two chiral binaphthyldisulfonate ligands and a bis(¦Ì-oxo)-dititanium(IV) core structure. The sulfonamide groups of the ligands and water are necessary for the catalysis, as they may stabilize the catalytically active complex through hydrogen bonding. Various 2-methylcoumarans were obtained in up to greater than 99% yields and up to 97% enantiomeric excess under mild conditions.

ACS Catalysis published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C5H12O2, Synthetic Route of 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Xu, Hongjiao published the artcileSynthesis and preliminary antitumor activity evaluation of 17-(5-(substituted cinnamamido)pentylamino)-17-demethoxygeldanamycin derivatives as potent Hsp90 Inhibitors, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid, the publication is Youji Huaxue (2015), 35(10), 2125-2134, database is CAplus.

Geldanamcyin (GA) was the first potent inhibitor of heat shock protein 90 (Hsp90) from natural products. However, its clin. application was limited by the unwanted hepatotoxicity. Our previous studies on the structure-activity relationships of GA derivatives indicated that the introduction of hepatoprotective cinnamoyl group via an alkyldiamino linker decreased the hepatotoxicity evidently. In this study, using pentyldiamine as the linker, twenty-six 17-(5-(substituted cinnamamido)pentylamino)-17-demethoxygeldanamycins were designed and synthesized as the inhibitors of Hsp90. All the compounds showed potent antitumor activities against human breast cancer cell line MDA-MB-231 with IC₅₀ ranging from 0.12 to 1 ¦Ìmol¡¤L^-1. Particularly, 17-(5-(cinnamamido)pentylamino)-17-demethoxygeldanamycin and 17-(5-(2,5-methoxycinn-amamido)pentylamino)-17-demethoxygeldanamycin were proved to be the most potent compounds (IC₅₀ = 0.12 ¦Ìmol¡¤L^-1), more active than the pos. control 17-N-allylamino-17-demethoxygeldanamycin (17-AAG) (IC₅₀ = 0.27 ¦Ìmol¡¤L^-1) and showed lower hepatotoxicity. Addnl., the preliminary structure-activity relationships among these newly synthesized congeners were briefly discussed, which should provide valuable basis for the structure optimization of GA-type Hsp90 inhibitors and antitumor lead compounds

Youji Huaxue published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C8H10S, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Wu, Yunfei published the artcileSynthesis of novel 17-[3,6-dioxa-8-N-(substituted cinnamoyl)-octanediamino]-17-demethoxygeldanamycin derivatives, Related Products of catalysis-chemistry, the publication is Youji Huaxue (2014), 34(9), 1870-1874, database is CAplus.

Twenty six new 17-[3,6-dioxa-8-N-(substituted cinnamoyl)octanediamino]-17-demethoxygeldanamycins were designed, synthesized and evaluated for their cytotoxicities against growth of human breast cancer cell line MDA-MB-231 and binding affinities to heat shock protein 90 (Hsp90). Among these derivatives, 17-(3,6-dioxa-8-N-((E)-3-(3,5-dimethoxyphenyl)acrylamido)octanediamino)-17-demethoxygeldanamycin, was identified as the most potent one (IC₅₀=1.5 ¦Ìmol/L, K_d=1.14 ¦Ìmol/L). Addnl., influence of substitutions at the cinnamoyl group on the bioactivities of this type of Geldanamycin (GA) derivatives was discussed. This study was anticipated to provide reference for the further structure modifications of GA for developing antitumor agents.

Youji Huaxue published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C8H10BNO3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Mao, Zhenkun published the artcileStrong hydrophilic monolithic column functionalized with amphiphilic benzyl quinine for capillary electrochromatography and application in pharmaceutical analysis, Safety of 1,1-Dimethylthiourea, the publication is Journal of Chromatography A (2020), 461031, database is CAplus and MEDLINE.

An innovative strong hydrophilic organic polymer monolithic column of poly(N-benzylquininium chloride-co-1, 3, 5-triacryloylhexahydro-1, 3, 5-triazine) (poly(NBQ-co-TAT)) has been successfully synthesized through in situ copolymerization for capillary electrochromatog. The amphiphilic monomer NBQ and the strong polar crosslinker TAT are firstly used in hydrophilic electrochromatog. by taking advantage of the exhibition of hydrophilicity at lower levels of organic solvent and ease formation of porous structure. The monolithic column poly(NBQ-co-TAT) shows powerful hydrophilic selectivity with mobile phase containing more than 60% organic solvent. The introduction of NBQ and TAT enlarges the sources of functional monomers and crosslinkers for HILIC. Due to the presence of the pos. charged group in NBQ, an anodic electroosmotic flow is generated with the change of pH values from 2.0 to 12.0. The monolithic column was used for the separations of thioureas, phenols, xanthines, nucleobases, acidic substances and pharmaceuticals. The highest column efficiency for N, N¡ä-dimethylthiourea is 1.15 ¡Á 10⁵ N m^-1. The application of the monolithic column for a real sample, cytochrome C digestion indicates its great potential in practical application.

Journal of Chromatography A published new progress about 6972-05-0. 6972-05-0 belongs to catalysis-chemistry, auxiliary class Thiourea,Amine,Aliphatic hydrocarbon chain,Amide, name is 1,1-Dimethylthiourea, and the molecular formula is C3H8N2S, Safety of 1,1-Dimethylthiourea.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Wang, Yiheng published the artcileSynthesis of an oxygen-linked germinal frustrated Lewis pair and its application in small molecule activation, COA of Formula: C18H23OP, the publication is RSC Advances (2018), 8(46), 26271-26276, database is CAplus and MEDLINE.

Reaction of Mes₂P(O)Li with (C₆F₅)₂BCl gave access to an oxygen-linked germinal intramol. frustrated Lewis pair Mes₂P(O)B(C₆F₅)₂ (1). Compound 1 is stable at room temperature and only decomposes when heated to 90¡ã. NMR anal. and theor. anal. revealed the frustrated nature between the boron and phosphorus centers. Compound 1 shows typical frustrated Lewis pair reactivity when treated with dihydrogen, carbon dioxide, alkyne and alkene. The reaction of 1 with isoprene resulted in selective formation of 3,4-phosphoryl/boryl addition product 8.

RSC Advances published new progress about 23897-16-7. 23897-16-7 belongs to catalysis-chemistry, auxiliary class Aryl phosphine ligand,Mono-phosphine Ligands, name is Dimesitylphosphine oxide, and the molecular formula is C19H17N2NaO4S, COA of Formula: C18H23OP.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Pei, Jin-Feng published the artcilePhoP- and GlnR-mediated regulation of metK transcription and its impact upon S-adenosyl-methionine biosynthesis in Saccharopolyspora erythraea, Product Details of C5H11NO2S, the publication is Microbial Cell Factories (2022), 21(1), 120, database is CAplus and MEDLINE.

Erythromycin A (Er A) has a broad antibacterial effect and is a source of erythromycin derivatives Methylation of erythromycin C (Er C), catalyzed by S-adenosyl-methionine (SAM)-dependent O-methyltransferase EryG, is the key final step in Er A biosynthesis. Er A biosynthesis, including EryG production, is regulated by the phosphate response factor PhoP and the nitrogen response factor GlnR. However, the regulatory effect of these proteins upon S-adenosyl-methionine synthetase (MetK) production is unknown. In this study, we used bioinformatics approaches to identify metK (SACE_3900), which codes for S-adenosyl-methionine synthetase (MetK). Electrophoretic mobility shift assays (EMSAs) revealed that PhoP and GlnR directly interact with the promoter of metK, and quant. PCR (RT-qPCR) confirmed that each protein pos. regulated metK transcription. Moreover, intracellular SAM was increased upon overexpression of either phoP or glnR under phosphate or nitrogen limited conditions, resp. Finally, both the production of Er A and the transformation ratio from Er C to Er A increased upon phoP overexpression, but surprisingly, not upon glnR overexpression. Manipulating the phosphate and nitrogen response factors, PhoP and GlnR provides a novel strategy for increasing the yield of SAM and the production of Er A in Saccharopolyspora erythraea .

Microbial Cell Factories published new progress about 63-68-3. 63-68-3 belongs to catalysis-chemistry, auxiliary class Natural product, name is (S)-2-Amino-4-(methylthio)butanoic acid, and the molecular formula is C5H11NO2S, Product Details of C5H11NO2S.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Ren, Jie published the artcileDesign, synthesis, and biological evaluation of oxazolidone derivatives as highly potent N-acylethanolamine acid amidase (NAAA) inhibitors, Formula: C15H14O3, the publication is RSC Advances (2017), 7(21), 12455-12463, database is CAplus.

N-Acylethanolamine-hydrolyzing acid amidase (NAAA) is a lysosomal enzyme that catalyzes the hydrolysis of endogenous fatty acid ethanolamides (FAEs), such as N-palmitoylethanolamide (PEA). PEA exhibits anti-inflammatory and analgesic activities by engaging peroxisome proliferator-activated receptor ¦Á (PPAR-¦Á). Preventing PEA degradation by inhibition of NAAA has been proposed as a novel strategy for the treatment of inflammation and pain. In the present study, we reported the discovery of the oxazolidone derivative as a novel scaffold for NAAA inhibitors, and studied the structure-activity relationship (SAR) by modification of the side chain and terminal lipophilic substituents. The results showed that the link chain length of C5, straight and saturated linkages were the preferred shape patterns for NAAA inhibition. Several nanomolar NAAA inhibitors were described, including 2f, 3h, 3i and 3j with IC₅₀ values of 270 nM, 150 nM, 100 nM and 190 nM, resp. Enzymic degradation studies suggested that 2f inhibited NAAA in a selective, noncompetitive and reversible pattern. Moreover, 2f showed high anti-inflammatory and analgesic activities after systemic and oral administration.

RSC Advances published new progress about 1860-58-8. 1860-58-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2-(3-(Benzyloxy)phenyl)acetic acid, and the molecular formula is C15H14O3, Formula: C15H14O3.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Zhang, Shanxue published the artcileElectrochemical Benzylic C(sp³)-H Isothiocyanation, Related Products of catalysis-chemistry, the publication is Organic Letters (2022), 24(8), 1742-1746, database is CAplus and MEDLINE.

Selective C(sp³)-H isothiocyanation represents a significant strategy for the synthesis of isothiocyanate derivatives Herein, the authors report an electrochem. benzylic isothiocyanation in a highly chemo- and site-selective manner under external oxidant-free conditions. The high chemoselectivity is attributed to the facile in-situ isomerization of benzylic thiocyanates to isothiocyanates. Notably, the method exhibits high functional group compatibility and is suitable for late-stage functionalization of bioactive mols.

Organic Letters published new progress about 457-68-1. 457-68-1 belongs to catalysis-chemistry, auxiliary class Fluoride,Benzene, name is Bis(4-fluorophenyl)methane, and the molecular formula is C14H26O2, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Qiao, Jingxin published the artcileSARS-CoV-2 M^pro inhibitors with antiviral activity in a transgenic mouse model, Name: (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, the publication is Science (Washington, DC, United States) (2021), 371(6536), 1374-1378, database is CAplus and MEDLINE.

The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continually poses serious threats to global public health. The main protease (M^pro) of SARS-CoV-2 plays a central role in viral replication. We designed and synthesized 32 new bicycloproline-containing M^pro inhibitors derived from either boceprevir or telaprevir, both of which are approved antivirals. All compounds inhibited SARS-CoV-2 M^pro activity in vitro, with 50% inhibitory concentration values ranging from 7.6 to 748.5 nM. The cocrystal structure of M^pro in complex with MI-23, one of the most potent compounds, revealed its interaction mode. Two compounds (MI-09 and MI-30) showed excellent antiviral activity in cell-based assays. In a transgenic mouse model of SARS-CoV-2 infection, oral or i.p. treatment with MI-09 or MI-30 significantly reduced lung viral loads and lung lesions. Both also displayed good pharmacokinetic properties and safety in rats.

Science (Washington, DC, United States) published new progress about 16909-09-4. 16909-09-4 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Benzene,Ether, name is (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, and the molecular formula is C11H12O4, Name: (E)-3-(2,4-Dimethoxyphenyl)acrylic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Cao, Jiawei published the artcilePreparation and multiple applications of integrated Zn-Al layered double hydroxide@polydopamine nanocomposites, Recommanded Product: 3-(Trimethoxysilyl)propan-1-amine, the publication is Materials Today Communications (2022), 103650, database is CAplus.

The preparation and application of inorganic-organic hybrid nanomaterials is a hot research topic at present. Herein, we combined Zn-Al layered double hydroxide (Zn-Al LDH) with mesoporous polydopamine (MPDA) to prepare two integrated Zn-Al LDH@MPDA nanocomposites under the modification of linker (1,3,5-benzoyl chloride (TMC) or (3-aminopropyl) trimethoxysilane (APTMS)), namely Composite T (modified by TMC) and Composite A (modified by APTMS), which were then evaluated for dye adsorption, adriamycin hydrochloride (DOX) loading, photothermal conversion experiment, and antibacterial test. The characterization results showed that MPDA can be successfully loaded on Zn-Al LDH with the modification of the two linkers, but the sp. surface area, pore-volume, average pore size, and electronegativity of Composite T were all higher than those of composite A, thus being more advantageous in adsorption of cationic dye. Composite T possesses a high loading capacity for DOX, whose loading efficiency and encapsulation efficiency are 478.3% and 95.7%, resp. In addition, Composite T also shows a high photothermal conversion efficiency of 27.9%. Furthermore, Composite T exhibits excellent antibacterial activity against Escherichia coli (E. coli) and Staphylococus aureus (S. aureus). Therefore, the designed Zn-Al LDH@MPDA nanocomposites would be a promising candidate for a myriad of industrial application fields.

Materials Today Communications published new progress about 13822-56-5. 13822-56-5 belongs to catalysis-chemistry, auxiliary class Organic Silicones, name is 3-(Trimethoxysilyl)propan-1-amine, and the molecular formula is C6H17NO3Si, Recommanded Product: 3-(Trimethoxysilyl)propan-1-amine.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia