Month: October 2022

Gao, Qiongqiong; Zhang, Jing; Chen, Chen; Chen, Menglin; Sun, Peng; Du, Wei; Zhang, Shengchang; Liu, Ying; Zhang, Rui; Bai, Mei; Fan, Changchun; Wu, Jibiao; Men, Tongyi; Jiang, Xinyi published the artcile< In Situ Mannosylated Nanotrinity-Mediated Macrophage Remodeling Combats Candida albicans Infection>, Recommanded Product: 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate, the main research area is insitu mannosylated Nanotrinity Mediated macrophage remodeling combats candida albicans; Candida albicans; chitosan oligosaccharides; imatinib; macrophage polarization; mannosylated nanotrinity.

Deep Candida albicans infection is one of the major causes of death in immunosuppressed hosts. Remodeling macrophages to phenotype M1 can decrease fungus burden and facilitate combating C. albicans under an immunosuppressive state. In this study, a nanotrinity was exploited to direct fungicidal macrophage polarization by leveraging the regulation pathways in macrophage redifferentiation. Conventional chemotherapeutic imatinib, which can abrogate M2 macrophage polarization via “”shutting off”” the STAT6 phosphorylation pathway, was encapsulated in biodegradable polymeric nanoparticles. In house-customized dual functional mannosylated chitosan oligosaccharides were then coated on the surface of the imatinib-laden nanoparticles, and thus, a mannosylated nanotrinity was achieved with ternary functions for macrophage remodeling: (i) imatinib-blocked STAT6 phosphorylation pathway for decreasing M2 macrophage population; (ii) chitosan oligosaccharides-mediated TLR-4 pathway activation that could promote macrophage redifferentiation to M1 phenotype; (iii) mannose motif-enhanced macrophage targeting. After physiochem. characterization, regulatory effects of the mannosylated nanotrinity on macrophages and the anti-C. albicans efficacy were evaluated at the cellular level and animal level, resp. The results demonstrated that our mannosylated nanotrinity could efficiently induce macrophage polarization toward the M1 phenotype, decrease M2 phenotype production, and markedly lessen fungus burden and increased the median survival time of mice infected with C. albicans. Therefore, the mannosylated nanotrinity developed in this study could significantly induce macrophage remodeling in situ by the two-pronged process, “”turning on”” M1 phenotype polarization meanwhile “”shutting off”” M2 phenotype polarization, and thus allowed to eradicate C. albicans infection.

ACS Nano published new progress about Candida albicans. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Recommanded Product: 2-(Bis(2-chloroethyl)amino)-1,3,2-oxazaphosphinane 2-oxide hydrate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Li, Na; Liu, Dan; Dai, Jiang-Kun; Wang, Jin-Yi; Wang, Jun-Ru published the artcile< Synthesis and in vitro antibacterial activity of quaternized 10-methoxycanthin-6-one derivatives>, Category: chlorides-buliding-blocks, the main research area is benzyl methoxycanthinone preparation agrochem antibacterial activity SAR; 10-methoxycanthin-6-one; SARs; antibacterial; quaternization.

Background: Based on our previous work, we found that 10-methoxycanthin-6-one displayed potential antibacterial activity and quaternization was an available method for increasing the antibacterial activity. Here, we explored the antibacterial activity of quaternized 10-methoxy canthin-6-one derivatives Methods and Results: Twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by the double dilution method. Moreover, the structure-activity relationships (SARs) were carefully summarized in order to guide the development of antibacterial canthin-6-one agents. Two highly active compounds displayed 8-fold superiority (MIC = 3.91 μg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae compared to agrochem. streptomycin sulfate, and showed potential activity against B. cereus. Moreover, these two compounds exhibited good “”drug-like”” properties, low cytotoxicity, and no inhibition on seed germination. Conclusions: This work provides two new effective quaternized canthin-6-one derivatives as candidate bactericide, promoting the development of natural-sourced bactericides and preservatives.

Molecules published new progress about Agrochemical antibacterial agents. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Misik, Miroslav; Nersesyan, Armen; Kment, Michael; Ernst, Benjamin; Setayesh, Tahereh; Ferk, Franziska; Holzmann, Klaus; Krupitza, Georg; Knasmueller, Siegfried published the artcile< Micronucleus assays with the human derived liver cell line (Huh6): A promising approach to reduce the use of laboratory animals in genetic toxicology>, Reference of 6055-19-2, the main research area is micronucleus human liver cell line genetic toxicol; Cytokinesis-block micronucleus assay; Genotoxicity; Huh6; In vitro assay; Micronucleus; Sensitivity; Specificity.

The inadequate representation of enzymes which catalyze the activation/detoxification of xenobiotics in cells that are currently used in genotoxicity testing of chems. leads to a high number of false pos. results and the number of follow up studies with rodents could be reduced by use of more reliable in vitro models. We found earlier that several xenobiotic drug metabolizing enzymes are represented in the human derived liver cell line Huh6 and developed a protocol for micronucleus (MN) experiments which is in agreement with the current OECD guideline. This protocol was used to test 23 genotoxic and non-genotoxic reference chems.; based on these results and of earlier findings (with 9 chems.) we calculated the predictive value of the assay for the detection of genotoxic carcinogens. We found a sensitivity of 80% and a specificity of 94% for a total number of 32 chems.; comparisons with results obtained with other in vitro assays show that the validity of MN tests with Huh6 is higher as that of other exptl. models. These results are promising and indicate that the use of Huh6 cells in genetic toxicol. may contribute to the reduction of the use of laboratory rodents; further exptl. work to confirm this assumption is warranted.

Food and Chemical Toxicology published new progress about Cytokinesis. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Garcia-Monzon, Irma; Borges-Gonzalez, Jorge; Martin, Tomas published the artcile< Solid-Supported Tetrahydropyran-Based Hybrid Dipeptide Catalysts for Michael Addition of Aldehydes to Nitrostyrenes>, Computed Properties of 5153-70-8, the main research area is tetrahydropyran dipeptide catalyst solid support aldehyde nitrostyrene michael addition.

The heterogenization of homogeneous catalysts onto a solid support is a step towards a more sustainable chem. The recovery and reuse of catalysts is extremely important from a practical, economic and environmental point of view. In this regards, we report a series of polymer-supported tetrahydropyran-based hybrid dipeptides that serve as active catalysts for the enantioselective Michael addition of aldehydes to β-nitrostyrenes. These supported catalysts have been designed considering the optimal anchor position and orientation between the catalyst and the solid support. Addnl., the influence of the linker length on the catalytic efficiency was studied. The catalysts allowed the transformation of a variety of substrates in 76-98% yield and with 94-97% enantiomeric excess. Detailed deactivation studies have provided important information, which allows to increase the useful life of these immobilized catalysts.

Advanced Synthesis & Catalysis published new progress about Asymmetric catalysis. 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, Computed Properties of 5153-70-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhao, Jian; Li, Shuang; Wang, Xinyi; Xu, Gang; Gou, Shaohua published the artcile< Dinuclear Organoruthenium Complexes Exhibiting Antiproliferative Activity through DNA Damage and a Reactive-Oxygen-Species-Mediated Endoplasmic Reticulum Stress Pathway>, Synthetic Route of 67421-02-7, the main research area is dinuclear organoruthenium complex preparation cancer DNA.

Subtle ligand modifications on ruthenium arene complexes can lead to different mechanisms of action and result in significant changes in the anticancer efficacy. Herein, four novel dinuclear ruthenium(II) arene complexes were designed and prepared In vitro tests indicated that complexes 1-3 displayed moderate antiproliferative activity against the tested cancer cells, while the cytotoxicity of complex 4 is superior or comparable to that of cisplatin. Further studies indicated that complexes 1-4 induce cell death through DNA interaction and a reactive-oxygen-species-mediated endoplasmic reticulum (ER) stress pathway, which is the first example of an organometallic ruthenium(II) arene complex to induce ER stress as well as DNA interaction. This kind of dinuclear ruthenium(II) arene complex has unique biol. characteristics and is a promising model for new anticancer drug development.

Inorganic Chemistry published new progress about Antiproliferative agents. 67421-02-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C24H36Cl4Ru2, Synthetic Route of 67421-02-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ohba, Mai; Oka, Tomoichiro; Ando, Takayuki; Arahata, Saori; Ikegaya, Asaka; Takagi, Hirotaka; Ogo, Naohisa; Owada, Kazuhiro; Kawamori, Fumihiko; Wang, Qiuhong; Saif, Linda J.; Asai, Akira published the artcile< Discovery and synthesis of heterocyclic carboxamide derivatives as potent anti-norovirus agents>, Application of C5H2Cl2O2S, the main research area is heterocyclic carboxamide preparation SAR antiviral.

In this study, synthesis, anti-norovirus activity, and structure-activity relationship (SAR) of a series of heterocyclic carboxamide derivatives I (R3 = 2-thienyl, 2-furyl, 2-thiazolyl, etc.; R4 = H, 6-Cl, 4-Br, etc.) has been described. Heterocyclic carboxamide I (R3 = 5-bromo-thiophen-2-yl; R4 = 6-F) (50% effective concentration (EC50)= 37 μM) was identified using the cytopathic effect reduction assay by the author’s screening campaign. Initial SAR studies suggested the importance of halogen substituents on the heterocyclic scaffold and identified 3,5-di-bromo-thiophene derivative (EC50 = 24 μM) and 4,6-di-benzothiazole derivative (EC50 = 5.6 μM) as more potent inhibitors than I (R3 = 5-bromo-thiophen-2-yl; R4 = 6-F). Moreover, their hybrid compound, 3,5-di-bromo-thiophen-4,6-di-fluoro-benzothiazole, showed the most potent anti-norovirus activity with a EC50 value of 0.53 μM. Further investigation suggested that the hybrid compound might inhibit intracellular viral replication or the late stage of viral infection.

Chemical & Pharmaceutical Bulletin published new progress about Antiviral agents. 31166-29-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C5H2Cl2O2S, Application of C5H2Cl2O2S.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Riley, Kevin E.; Murray, Jane S.; Fanfrlik, Jindrich; Rezac, Jan; Sola, Ricardo J.; Concha, Monica C.; Ramos, Felix M.; Politzer, Peter published the artcile< Halogen bond tunability I: the effects of aromatic fluorine substitution on the strengths of halogen-bonding interactions involving chlorine, bromine, and iodine>, Related Products of 1435-43-4, the main research area is halogen bond tunability iodine aromatic fluorine substitution strength bonding; chlorine bromine halogen bond.

In the past several years, halogen bonds are relevant in crystal engineering and biomedical applications. One of the reasons for the utility of these types of noncovalent interactions in the development of, for example, pharmaceutical ligands is that their strengths and geometric properties are very tunable. That is, substitution of atoms or chem. groups in the vicinity of a halogen can have a very strong effect on the strength of the halogen bond. The authors study halogen-bonding interactions involving aromatically-bound halogens (Cl, Br, and I) and a carbonyl oxygen. The properties of these halogen bonds are modulated by substitution of aromatic hydrogens with fluorines, which are very electroneg. These types of substitutions have dramatic effects on the strengths of the halogen bonds, leading to interactions that can be up to 100% stronger. Very good correlations are obtained between the interaction energies and the magnitudes of the pos. electrostatic potentials (σ-holes) on the halogens. The substitution of fluorines in systems containing smaller halogens results in electrostatic potentials resembling those of systems with larger halogens, with correspondingly stronger interaction energies. Also aromatic fluorine substitutions affect the optimal geometries of the halogen-bonded complexes, often as the result of secondary interactions.

Journal of Molecular Modeling published new progress about Aryl halides Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), PROC (Process). 1435-43-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H3ClF2, Related Products of 1435-43-4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhang, Yuanyuan; Liang, Yaoyu; Zhao, Xiaodan published the artcile< Chiral Selenide-Catalyzed, Highly Regio- and Enantioselective Intermolecular Thioarylation of Alkenes with Phenols>, Related Products of 128-09-6, the main research area is chiral phenol preparation regioselective enantioselective diastereoselective; alkene phenol thiosuccinimide three component thioarylation chiral selenide catalyst.

Enantioselective electrophilic three-component thioarylation of alkenes by chiral selenide catalysis with free phenols as arylating sources is disclosed. A variety of chiral phenols, e.g., I, were prepared in high regio-, enantio-, and diastereoselectivities. Mechanistic studies revealed that this transformation went through carbon nucleophilic attack to give the products rather than the process of intramol. rearrangement of phenolic ether intermediates. The application of this organocatalytic method in the alkylation of methoxy-substituted benzenes elucidated its generality.

ACS Catalysis published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Related Products of 128-09-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Suri Babu, Undamatla; Singam, Maneesh Kumar Reddy; Kumar, Muniganti Naveen; Nanubolu, Jagadeesh Babu; Sridhar Reddy, Maddi published the artcile< Palladium-Catalyzed Carbo-Aminative Cyclization of 1,6-Enynes: Access to Naphthyridinone Derivatives>, Formula: C9H5ClO2, the main research area is naphthyridinone preparation; enyne iodoaniline carbo aminative cyclization palladium catalyst.

A general approach to naphthyridinones I [R = H, 8-Me, 7-F, etc.; Ar = Ph, 4-MeC6H4, Bn, etc.; Ar1 = Ph, 4-MeC6H4, 2-thienyl, etc.] was described via Pd-catalyzed annulation of 1,6-enynes with 2-iodoanilines. This protocol represents a rare carbo-aminative annulative cyclization via 6-endo-trig mode, subduing the well documented exo-trig/dig cyclizations. Regioselective aryl palladation of alkyne followed by Heck type intramol. coupling before isomerization were key in realizing this cascade.

Organic Letters published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 3240-10-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H5ClO2, Formula: C9H5ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Liu, Qiyu; Zhou, Liang; Fan, Di; Guan, Mingzhao; Ma, Qiaozhi; Li, Song; Ouyang, Xinping; Qiu, Xueqing; Fan, Wei published the artcile< Adsorption-Enhanced Glucan Oligomer Production from Cellulose Hydrolysis over Hyper-Cross-Linked Polymer in Molten Salt Hydrate>, SDS of cas: 1592-20-7, the main research area is adsorption glucan oligomer cellulose molten salt hydrate; cellulose; glucan oligomer; hydrolysis; hyper-cross-linked polymer; reactive adsorption.

Selective saccharification of cellulose into glucose is a critical step for utilization of lignocellulosic biomass. Molten salt hydrates (MSHs) have shown promising performance in selectively converting cellulose into glucose because of the high solubility of cellulose in the solvent. However, the separation of formed glucose from the MSHs is still a grand challenge. To address this issue, we developed a two-step process, where crystalline cellulose is hydrolyzed into short-chain glucan oligomers in MSHs followed by separation and subsequent hydrolysis of the formed oligomers into glucose under mild conditions. The two-step method provides an easy separation for glucan oligomers from the MSHs without sacrificing the selectivity to glucose. Application of the method for crystalline cellulose is, however, limited to a relatively low concentration, 26.2 mg/mL, because of the formation of byproducts in the MSH that facilitate oligomers degradation In this work, reactive adsorption was employed to in situ remove the byproducts formed during cellulose hydrolysis in the MSH. It was found that hyper-crosslinked polymer (HCP) made from the polymerization of 4-vinylbenzyl chloride and divinylbenzene can selectively adsorb 5-hydroxymethylfurfural (5-HMF) and levulinic acid (LA) while showing negligible sugar adsorption in both water and the MSH. With the reactive adsorption approach, byproducts including 5-HMF and LA were removed from the reaction media under reaction conditions, and their neg. effects on oligomer degradation were inhibited. In the presence of the HCP, the obtained glucan oligomer concentration was enhanced from less than 54.2 to 247.1 mg mL-1 when the weight ratio of cellulose was increased to MSH from 1:60 to 1:4, exhibiting an oligomer yield of 69.5%. The HCP can be effectively separated from the reaction media by filtration and regenerated by oxidation with hydrogen peroxide. Application of reactive adsorption with HCP for cellulose hydrolysis in the MSH provides a promising method to produce glucan oligomers and glucose with an improved yield and efficiency.

ACS Applied Materials & Interfaces published new progress about Adsorbents. 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, SDS of cas: 1592-20-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics