Category: 74317-85-4

Yang, Fen-Fen published the artcileSynthesis and antibacterial activity studies in vitro of indirubin-3′-monoximes, COA of Formula: C8H7BrO3, the main research area is indirubin monoxime preparation antibacterial activity.

Multi-drug-resistant microbial pathogens are a serious global health problem. New compounds with antibacterial activity serve as good candidates for developing novel antibacterial drugs which is very urgent and important. In this work, based on the unique scaffold of indirubin, an active ingredient of traditional Chinese medicine formulation Danggui Luhui Wan, we synthesized 29 indirubin-3′-monoximes and preliminarily evaluated their antibacterial activities. The antibacterial activity results demonstrated that the synthesized indirubin-3′-monoximes 5a-5z and 5aa-5ad displayed good potency against S. aureus ATCC25923 (MIC = 0.4-25.6 μg mL-1). Among them, we found that the 5-F, 5-Cl and 7-CF3 substituted indirubin-3′;-monoximes 5r, 5s and 5aa also showed better antibacterial efficiency for S. aureus (MICs up to 0.4 μg mL-1) than the prototype natural product indirubin (MIC = 32 μg mL-1). More importantly, indirubin-3′-monoxime 5aa has certain synergistic effect with levofloxacin against clinic multidrug-resistant S. aureus (fractional inhibitory concentration index: 0.375). In addition, relevant experiments including electron microscopy observations, PI staining and the leakage of extracellular potassium ions and nucleic acid (260 nm) have been performed after treating S. aureus with indirubin-3′-monoxime 5aa, and the results revealed that indirubin-3′-monoximes could increase the cell membrane permeability of S. aureus. Although indirubin-3′-monoxime 5aa showed some cytotoxicity toward SH-SY5Y cells relative to compounds 5r and 5s, the skin irritation test of male mice after shaving showed that compound 5aa at a concentration of 12.8 μg mL-1 had no toxicity to mouse skin, and it could be used as a leading compound for skin antibacterial drugs.

RSC Advances published new progress about Antibacterial agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, COA of Formula: C8H7BrO3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Moreno-Sanz, Guillermo published the artcileSynthesis and Structure-Activity Relationship Studies of O-Biphenyl-3-yl Carbamates as Peripherally Restricted Fatty Acid Amide Hydrolase Inhibitors, COA of Formula: C8H7BrO3, the main research area is biphenyl carbamate preparation peripherally restricted FAAH inhibitor SAR; URB937 analog brain impermeant fatty acid amide hydrolase inhibitor; restricted access central nervous system biphenyl carbamate derivative.

The peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor URB937 (I, cyclohexylcarbamic acid 3′-carbamoyl-6-hydroxybiphenyl-3-yl ester) is extruded from the brain and spinal cord by the Abcg2 efflux transporter. Despite its inability to enter the central nervous system (CNS), I exerts profound antinociceptive effects in mice and rats, which result from the inhibition of FAAH in peripheral tissues and the consequent enhancement of anandamide signaling at CB1 cannabinoid receptors localized on sensory nerve endings. In the present study, we examined the structure-activity relationships (SAR) for the biphenyl region of compound I, focusing on the carbamoyl and hydroxyl groups in the distal and proximal Ph rings. Our SAR studies generated a new series of peripherally restricted FAAH inhibitors and identified compound II (cyclohexylcarbamic acid 3′-carbamoyl-5-hydroxybiphenyl-3-yl ester) as the most potent brain-impermeant FAAH inhibitor disclosed to date.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, COA of Formula: C8H7BrO3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kondo, Hiroki published the artcileBranch-Selective Allylic C-H Carboxylation of Terminal Alkenes by Pd/sox Catalyst, SDS of cas: 74317-85-4, the main research area is regioselective carboxylation terminal alkene carboxylic acid palladium SOX catalyst; branched allylic ester preparation.

A ligand-controlled branch-selective allylic C-H carboxylation through Pd catalysis is described. The developed catalytic system, which consists of Pd(OAc)2, sulfoxide-oxazoline (sox) as a ligand and benzoquinone as an oxidant, couples terminal alkenes and carboxylic acids to furnish the corresponding branched allylic esters with high regioselectivity.

Organic Letters published new progress about C-H bond activation. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, SDS of cas: 74317-85-4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Nan published the artcileModification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci, Synthetic Route of 74317-85-4, the main research area is vancomycin resistant Enterococci 5 methylphenanthridium benzothiazoles FtsZ inhibitors; Antibacterial activity; Benzothiazolyl-5-methylphenanthridium; FtsZ inhibitors; Indolyl-5-methylphenanthridium; Mechanism of action.

The death caused by pathogenic bacteria has always been a severe threat to mankind. The prevalence of drug resistance among bacteria underscores an urgent goal for new antibacterial agents with novel mode of action. Here we first designed and synthesized a class of benzothiazolyl-5-methylphenanthridium derivatives and evaluated their antibacterial activity. On this basis, we further designed and synthesized another class of novel indolyl-5-methylphenanthridium derivatives by optimizing the benzothiazolyl-5-methylphenanthridium core and evaluated their antibacterial activity targeting the bacterial cell division protein FtsZ. The results showed that the indolyl-5-methylphenanthridium derivatives had greatly improved activity against various drug-resistant bacterial strains including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus (VRE). Among them, compound C5 displayed excellent antibacterial activity against susceptible (MIC = 1μg/mL), methicillin-resistant and clin. isolated S. aureus (MIC = 2μg/mL). With low hemolytic activity towards mice red blood cells, C5 exhibited good antibacterial effect in vivo in preliminary pharmacodynamic assay. More importantly, C5 was difficult to induce bacterial resistance. Further mechanism studies proved that C5 could inhibit bacterial cell division by promoting FtsZ polymerization, leading to disorderly polymerization and disordered knots. Therefore, our findings suggest that this class of novel indolyl-5-methylphenanthridium derivatives are promising for future antibacterial agents.

European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Synthetic Route of 74317-85-4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wang, Yi-Ting published the artcileNovel nucleocapsid protein-targeting phenanthridine inhibitors of SARS-CoV-2, COA of Formula: C8H7BrO3, the main research area is nucleocapsid protein phenanthridine inhibitor SARS CoV2 coronavirus COVID19; N-terminal domain; Nucleocapsid protein; Phenanthridine; SARS-CoV-2.

The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is unprecedented in human history. As a major structural protein, nucleocapsid protein (NPro) is critical to the replication of SARS-CoV-2. In this work, 17 NPro-targeting phenanthridine derivatives were rationally designed and synthesized, based on the crystal structure of NPro. Most of these compounds can interact with SARS-CoV-2 NPro tightly and inhibit the replication of SARS-CoV-2 in vitro. Compounds 12 and 16 exhibited the most potent anti-viral activities with 50% effective concentration values of 3.69 and 2.18μM, resp. Furthermore, site-directed mutagenesis of NPro and Surface Plasmon Resonance (SPR) assays revealed that 12 and 16 target N-terminal domain (NTD) of NPro by binding to Tyr109. This work found two potent anti-SARS-CoV-2 bioactive compounds and also indicated that SARS-CoV-2 NPro-NTD can be a target for new anti-virus agents.

European Journal of Medicinal Chemistry published new progress about Anticoronaviral agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, COA of Formula: C8H7BrO3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chen, Weixiong published the artcileDiscovery of highly potent SARS-CoV-2 Mpro inhibitors based on benzoisothiazolone scaffold, Formula: C8H7BrO3, the main research area is benzoisothiazolone scaffold SARSCoV2 coronavirus Mpro inhibitor COVID19; Benzoisothiazolone; COVID-19; Main protease inhibitors; SARS-CoV-2.

The COVID-19 pandemic has drastically impacted global economies and public health. Although vaccine development has been successful, it was not sufficient against more infectious mutant strains including the Delta variant indicating a need for alternative treatment strategies such as small mol. compound development. In this work, a series of SARS-CoV-2 main protease (Mpro) inhibitors were designed and tested based on the active compound from high-throughput diverse compound library screens. The most efficacious compound (16b-3) displayed potent SARS-CoV-2 Mpro inhibition with an IC50 value of 116 nM and selectivity against SARS-CoV-2 Mpro when compared to PLpro and RdRp. This new class of compounds could be used as potential leads for further optimization in anti COVID-19 drug discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoronaviral agents. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Formula: C8H7BrO3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Likai published the artcileEnantioselective Transfer Hydrogenation of Oxocarbenium Ions Enables Asymmetric Access to α-Substituted 1,3-Dihydroisobenzofurans, Recommanded Product: 2-Bromo-4-methoxybenzoic acid, the main research area is dihydroisobenzofuran preparation enantioselective; cyclic oxocarbenium ion ketal transfer hydrogenation.

Reported here is an efficient enantioselective transfer hydrogenation of cyclic oxocarbenium ions generated in situ through collapse of the corresponding acetal substrates. The asym. approach provides straightforward access to a variety of chiral α-aryl substituted 1,3-dihydroisobenzofurans in high yields with excellent enantioselectivities. α-Alkynyl substituted 1,3-dihydroisobenzofurans were also proved to be suitable substrates. In addition, when the reaction was performed at gram scale, the desired product was obtained in good yields with excellent enantioselectivity.

Synthesis published new progress about Carbocations, carbenium. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Recommanded Product: 2-Bromo-4-methoxybenzoic acid.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Trost, Barry M. published the artcileSulfones as Synthetic Linchpins: Transition-Metal-Free sp3-sp2 and sp2-sp2 Cross-Couplings Between Geminal Bis(sulfones) and Organolithium Compounds, Application of 2-Bromo-4-methoxybenzoic acid, the main research area is substituted dihydronaphthalene preparation; geminal bis sulfone organolithium compound coupling; cross-coupling; sulfones; synthesis design; transition-metal-free; umpolung.

A valuable umpolung strategy that highlights the ambiphilic nature of the bis(phenylsulfonyl)methyl synthons and demonstrates its utility as a synthetic linchpin is reported. Alkyl- and aryllithiums couple with the central carbon of the bis(phenylsulfonyl)methyl unit to ultimately generate trisubstituted alkenes I [R = H, 6-MeO, 7-F, etc.; R1 = n-Bu, Ph, (CH2)2C6H5, etc.], comprising formal sp3-sp2 and sp2-sp2 cross-couplings between organolithium reagents and bis(sulfones). This process occurs almost instantaneously at -78 °C in the absence of any transition metals. By developing this curious transformation, it has been demonstrated that bis(phenylsulfonyl)methane is a valuable synthetic linchpin, which can undergo two C-C bond-forming processes as an sp3-nucleophile, followed by a third C-C bond-forming reaction as an effective sp2-electrophile. This discovery significantly enhances the utility of this ubiquitous, but underutilized, linker group.

Chemistry – A European Journal published new progress about Acidity function, Hammett. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Application of 2-Bromo-4-methoxybenzoic acid.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Joshi-Pangu, Amruta published the artcileAcridinium-Based Photocatalysts: A Sustainable Option in Photoredox Catalysis, Category: bromides-buliding-blocks, the main research area is acridinium photoredox catalysis redox potential.

The emergence of visible light photoredox catalysis has enabled the productive use of lower energy radiation, leading to highly selective reaction platforms. Polypyridyl complexes of iridium and ruthenium have served as popular photocatalysts in recent years due to their long excited state lifetimes and useful redox windows, leading to the development of diverse photoredox-catalyzed transformations. The low abundances of Ir and Ru in the earth’s crust and, hence, cost make these catalysts nonsustainable and have limited their application in industrial-scale manufacturing Herein, we report a series of novel acridinium salts as alternatives to iridium photoredox catalysts and show their comparability to the ubiquitous [Ir(dF-CF3-ppy)2(dtbpy)](PF6).

Journal of Organic Chemistry published new progress about Half wave potential, redox. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhao, Nan published the artcileAsymmetric total synthesis of (+)-astellatol and (-)-astellatene, Related Products of bromides-buliding-blocks, the main research area is astellatol enantioselective preparation; astellatene enantioselective preparation.

The synthesis of (+)-astellatol, as well as the first total synthesis of (-)-astellatene was described. This work highlights a mercury(II)-catalyzed Grignard reaction, an intramol. Pauson-Khand reaction, a samarium(II)-mediated reductive radical 1,6-addition and a novel strategy for the synthesis of highly substituted trans-hydrindane natural products.

Organic Chemistry Frontiers published new progress about Enantioselective synthesis. 74317-85-4 belongs to class bromides-buliding-blocks, name is 2-Bromo-4-methoxybenzoic acid, and the molecular formula is C8H7BrO3, Related Products of bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary