Month: December 2022

Chen, Jing published the artcileA novel”turn-off”fluorescence assay based on acid-copper nanoclusters in deep eutectic solvent micelles for co-aggregation inducing fluorescence enhancement and its application, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride, the publication is Talanta (2021), 223(Part_1), 121731, database is CAplus and MEDLINE.

As mixtures, deep eutectic solvent (DES) is designability. By adjusting the long alkyl chain hydrogen bond acceptors (HBAs) or hydrogen bond donors (HBDs), the DES displays surfactant characteristics and can form micelles. Hence, a novel, simple, facile and green natural organic acids capped copper nanoclusters (Aci-CuNCs) was synthesized and the spectrum behavior of Aci-CuNCs in DES micelles was researched. It was found that the surfactant-like DES can form micellar co-aggregation with Aci-CuNCs, resulting in the fluorescence (FL) intensive of Aci-CuNCs increase. Corresponding performance of spectral properties of Aci-CuNCs in DES medium were systematically studied by fourier transform IR spectrometer, 3D FL spectroscopy, FL emission/excitation spectra, UV absorption spectroscopy. In the mechanism exploration part, on the one hand, the existence of micellar co-aggregation was confirmed by the conductivity, the mass effect of DES, dynamic light scattering and transmission electron microscopy. On the other hand, the influence of different kinds of DESs (types of HBAs/HBDs, molar ratio) and some possible factors (ionic strength and temperature) were discussed in detail to investigate the main driving forces for the formation of micellar co-aggregates. The results of mechanism exploration prove that the long alkyl chain of DES is amphiphilic which can form micellar co-aggregation with Aci-CuNCs through hydrogen bonding. The DES micelle provides Aci-CuNCs with a relatively stable and closed micro-environment which can effectively prevent collisions with water mols. and weakening of fluorescence intensity. On the basic of the above research, a “turn-off” fluorimetric method based on Aci-CuNCs in DES medium was applied for the determination of Fe³⁺. Under the optimum conditions, the assay worked in the Fe³⁺ concentration ranges from 1 to -20μM and had a detection limit of 0.0374μM. Method validation study illustrates the proposed system can provide a good accuracy, repeatability and stability conditions. Furthermore, the real sample anal. result demonstrates that no obvious matrix effect is found. As a consequence, the FL assays (Aci-CuNCs-based DES) composed of natural organic acid capped CuNCs and green solvent DES provides a simple, gentle and environmentally friendly method for the detection of iron ions.

Talanta published new progress about 23616-79-7. 23616-79-7 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst, name is N-Benzyl-N,N-dibutylbutan-1-aminium chloride, and the molecular formula is C19H34ClN, Safety of N-Benzyl-N,N-dibutylbutan-1-aminium chloride.

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

Hu, Yuhan published the artcileEnzyme-instructed self-assembly of peptide-drug conjugates in tear fluids for ocular drug delivery, Recommanded Product: 2-Chlorotrityl chloride, the publication is Journal of Controlled Release (2022), 261-271, database is CAplus and MEDLINE.

In vivo self-assembly of small mols. offers an excellent opportunity for targeted and long-term accumulation of a therapeutic agent at the lesion site. Here we demonstrate the strategy of enzyme-instructed self-assembly (EISA) by designing a phosphorylated peptide-drug (IBF-HYD-GFFpY) precursor through the ester bond to release active drugs at the target site. Meanwhile, the in vivo assembly can be achieved by the catalysis of alk. phosphatase (ALP) in the tear fluid for ocular drug delivery efficiently. The in vitro enzymic experiments indicate that the dephosphorylation of IBF-HYD-GFFpY occurs firstly with the yield of IBF-HYD-GFFY which subsequently self-assembles into the supramol. hydrogel to afford sustained drug release over 96 h. In the treatment of lipopolysaccharide (LPS)-activated Raw 264.7 macrophages, IBF-HYD-GFFpY exerts the more potent anti-inflammatory efficacy than that of free ibuprofen (IBF) at the concentration of 200 μM. Moreover, the aqueous solution of IBF-HYD-GFFpY via topical instillation hardly causes ocular irritation, and displays longer precorneal retention compared to the conventional eye drop formulation. In addition, in the in vivo study, a rabbit model of endotoxin-induced uveitis (EIU) evidences the comparable therapeutic efficacy of IBF-HYD-GFFpY eye drops with that of clin. used 0.1 wt% diclofenac (DIC) sodium eye drops by the reduction of macrophage and leukocyte influx. This work, in situ EISA in the tear microenvironment directing in vivo self-assembly of small mols., may guide a powerful approach for developing enzymic self-assembled mols. as an efficient delivery system of ocular drugs.

Journal of Controlled Release published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.

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

Chen, Rongxiang published the artcileCobalt-catalyzed decarboxylative oxyalkylation of styrenes with α-cyanoacid: Access to γ-ketonitriles, Related Products of chlorides-buliding-blocks, the publication is Tetrahedron Letters (2022), 153807, database is CAplus.

A cobalt-catalyzed decarboxylative oxyalkylation of styrenes ArCH=CH₂ (Ar = 3,4-dimethoxyphenyl, 2-naphthyl, 4-cyanophenyl, etc.) and (E)-prop-1-en-1-ylbenzene with α-cyanoacid has been established, leading to a variety of γ-ketonitriles ArC(O)CH₂CH₂CN and 3-methyl-4-oxo-4-phenylbutanenitrile in moderate yields. An α-Cyanoacid was applied as the nitrile sources. This methodol. was distinguished by operational simplicity, easily available starting materials and good functionality tolerance.

Tetrahedron Letters published new progress about 1263414-46-5. 1263414-46-5 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Alkenyl,Benzene, name is 4-Chloro-3-fluorostyrene, and the molecular formula is C8H6ClF, Related Products of chlorides-buliding-blocks.

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

Zhang, Xiao published the artcileDesign, Synthesis, and Synergistic Activity of Eight-Membered Oxabridge Neonicotinoid Analogues, Safety of 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Journal of Agricultural and Food Chemistry (2021), 69(10), 3005-3014, database is CAplus and MEDLINE.

Insecticide synergists are sought-after due to their potential in improving the pesticide control efficacy with a reduced dose of an active ingredient. We previously reported that a cis-configuration neonicotinoid (IPPA08) exhibited specific synergistic activity toward neonicotinoid insecticides. In this study, we synthesized a series of structural analogs of IPPA08 by converting the pyridyl moiety of IPPA08 into Ph groups, via facile double-Mannich condensation reactions between nitromethylene compounds and glutaraldehyde. All of the oxabridged neonicotinoid compounds were found to increase the toxicity of imidacloprid against Aphis craccivora. Notably, compound (I) at 0.75 mg/L lowered the LC₅₀ value of imidacloprid against A. craccivora by 6.54-fold, while a 3.50-fold reduction of the LC₅₀ value was observed for IPPA08. The results of bee toxicity test showed that compound I display selectivity in its effects on imidacloprid toxicity against the honey bee (Apis mellifera L.). In summary, replacing the pyridyl ring with a Ph ring was a viable approach to obtain a novel synergist with oxabridged moiety for neonicotinoid insecticides.

Journal of Agricultural and Food Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H17Br, Safety of 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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

Zhang, Xiao published the artcileDesign, Synthesis, and Synergistic Activity of Eight-Membered Oxabridge Neonicotinoid Analogues, Category: chlorides-buliding-blocks, the publication is Journal of Agricultural and Food Chemistry (2021), 69(10), 3005-3014, database is CAplus and MEDLINE.

Insecticide synergists are sought-after due to their potential in improving the pesticide control efficacy with a reduced dose of an active ingredient. We previously reported that a cis-configuration neonicotinoid (IPPA08) exhibited specific synergistic activity toward neonicotinoid insecticides. In this study, we synthesized a series of structural analogs of IPPA08 by converting the pyridyl moiety of IPPA08 into Ph groups, via facile double-Mannich condensation reactions between nitromethylene compounds and glutaraldehyde. All of the oxabridged neonicotinoid compounds were found to increase the toxicity of imidacloprid against Aphis craccivora. Notably, compound (I) at 0.75 mg/L lowered the LC₅₀ value of imidacloprid against A. craccivora by 6.54-fold, while a 3.50-fold reduction of the LC₅₀ value was observed for IPPA08. The results of bee toxicity test showed that compound I display selectivity in its effects on imidacloprid toxicity against the honey bee (Apis mellifera L.). In summary, replacing the pyridyl ring with a Ph ring was a viable approach to obtain a novel synergist with oxabridged moiety for neonicotinoid insecticides.

Journal of Agricultural and Food Chemistry published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C11H13N3, Category: chlorides-buliding-blocks.

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

He, Renbao published the artcileSynthesis of 2,4,5-trifluorobenacetic acid, Quality Control of 243139-71-1, the publication is Huagong Shengchan Yu Jishu (2011), 18(3), 4-6, database is CAplus.

The compound 2,4,5-trifluorobenzeneacetic acid was synthesized from 1,2,4-trifluorobenzene via chloromethylation, carbonylation and hydrolyzation. Results showed that the optimization synthesis condition of 2,4,5-trifluorobenzyl chloride were as follows: m (C₆H₃F₃):m (paraformaldehyde)=1.0:0.875-0.865, reaction time 10 h. And the optimization synthesis condition of 2,4,5-trifluorobenzeneacetic acid was m (C₇H₄F₃Cl): m (cat)=1:0.275-0.25 and the reaction temperature was 40°C, under this condition, the total yield was above 60%, the purity was above 99%. The proportion of reactants and dosage of catalyst were discussed.

Huagong Shengchan Yu Jishu published new progress about 243139-71-1. 243139-71-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 2,4,5-Trifluorobenzyl chloride, and the molecular formula is C7H4ClF3, Quality Control of 243139-71-1.

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

Liu, Jiwen published the artcileOptimization of GPR40 Agonists for Type 2 Diabetes, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 517-521, database is CAplus and MEDLINE.

GPR40 (FFA1 and FFAR1) has gained significant interest as a target for the treatment of type 2 diabetes. TAK-875 (1), a GPR40 agonist, lowered Hb A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patients in phase II clin. trials. We optimized phenylpropanoic acid derivatives as GPR40 agonists and identified AMG 837 (2) as a clin. candidate. Here we report our efforts in searching for structurally distinct back-ups for AMG 837. These efforts led to the identification of more polar GPR40 agonists, such as AM-4668 (10), that have improved potency, excellent pharmacokinetic properties across species, and min. central nervous system (CNS) penetration.

ACS Medicinal Chemistry Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

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

Li, Xuemin published the artcileQuantitative analysis of 2,3-dibromopropionyl chloride, Application of 2,3-Dibromopropionylchloride, the publication is Ranliao Yu Ranse (2011), 48(6), 56-59, database is CAplus.

An anal. method for a dye intermediate 2,3-dibromopropionyl chloride was established. The method was based on derivation of 2,3-dibromopropionyl chloride. 2,3-Dibromo-N-phenylpropanamide was almost quant. prepared from 2,3-dibromopropionyl chloride and aniline by amidation. The external standard calibration curve of 2,3-dibromo-N-phenylpropanamide was obtained by HPLC, thus the content of 2,3-dibromopropionyl chloride was determined The linear regression equation of the method was given, the liner correlation coefficient was 0.9997, the linear range was 0.1341-0.6707 mg/mL, the standard deviation was 0.005, the variation coefficient was 0.5%, and the recovery rate was 99.81%-100.05%.

Ranliao Yu Ranse published new progress about 18791-02-1. 18791-02-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 2,3-Dibromopropionylchloride, and the molecular formula is C3H3Br2ClO, Application of 2,3-Dibromopropionylchloride.

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

Li, Ziyong published the artcileSolvent-dependent and visible light-activated NIR photochromic dithienylethene modified by difluoroboron β-diketonates as fluorescent turn-on pH sensor, Related Products of chlorides-buliding-blocks, the publication is Dyes and Pigments (2019), 339-347, database is CAplus.

The development of near-IR (NIR) photochromic materials, particularly activated by visible light, are of increasing interest for their potential application in photoresponsive optoelectronics and functional bio-materials. Here, a novel D-DTE-A type dithienylethene NDB, which was modified by difluoroboron β-diketonate (BF₂bdk) and dimethylphenylamine (DMPA) moieties, has been developed. It exhibited solvent-dependent photophys. properties before irradiation, and the visible light-triggered NIR photochromic behavior with solvent-dependent features was only observed in Toluene. Moreover, it displayed intense fluorescent turn-on acid-sensing properties in less polar solvent [Toluene, Dichloromethane (DCM) and Et acetate (EA)] through the blockage of photoinduced electron transfer (PET) effect. Specially, NDB with photochromic inactivity in DCM could perform a unique gated photochromism in the presence of TFA/TEA.

Dyes and Pigments published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H14Cl2S2, Related Products of chlorides-buliding-blocks.

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

Li, Ziyong published the artcileSynthesis and properties of dithienylethene-functionalized switchable antibacterial agents, Formula: C15H14Cl2S2, the publication is Organic & Biomolecular Chemistry (2018), 16(38), 6988-6997, database is CAplus and MEDLINE.

Photopharmacol. involving azobenzene has offered a viable alternative for combating bacterial resistance. However, the degradation and potential toxicity of azobenzene limit its further study in vivo. Therefore, searching for an appropriate photoswitch for further clin. application is highly desirable. Herein a series of dithienylethene-functionalized switchable antibacterial agents have been designed and prepared by the introduction of the dithienylethene scaffold into fluoroquinolones. And it was found that these switchable antibacterial agents displayed good photochromism and fluorescence switching behaviors upon irradiation with UV/Vis light in DMSO. Surprisingly, methoxy-substituted dithienylethenes 3a and 3b exhibited fluorescence turn-on behavior. Furthermore, it was found that all of the open-isomers showed partial antibacterial activity on E. coli and S. aureus compared with the native drugs. Apart from 2a and 2b, the other switchable antibacterial agents showed a large difference in antibacterial activity on Gram-neg. E. coli between the open and closed forms, in which the antimicrobial activity of the ring-closed isomers for 1b and 3b was 16 times that of the corresponding ring-open isomers. DFT calculations showed that the ring-closed isomers of 1b and 3b presented a rigid “S-type” conformation, which may be conducive to forming more stable complexes with the DNA gyrase of E. coli.

Organic & Biomolecular Chemistry published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H14Cl2S2, Formula: C15H14Cl2S2.

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