Category: 32333-53-2

Oh, Keimei published the artcileSynthesis and structure-activity relationships of new pyrazole derivatives that induce triple response in Arabidopsis seedlings, Name: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Journal of Pesticide Science (Tokyo, Japan) (2019), 44(4), 233-241, database is CAplus and MEDLINE.

Twenty-seven analogs of pyrazole derivatives I (R¹ = Me, Ph, allyl, tert-butyl; R² = 2-fluorophenyl, 3-chloro-4-fluorophenyl, 4-phenylazo, etc.) were synthesized and subjected to structure-activity relationship studies on inducing the triple response in Arabidopsis seedlings. The compound I (R¹ = allyl; R² = 3,4-dichlorophenyl) (II) has been found to exhibit potent activity on inducing the triple response in Arabidopsis seedlings. Compound II (10μM) induced an exaggerated apical hook in Arabidopsis seedlings. The curvature of the hook of the Arabidopsis seedlings was found to be 300 ± 23°, while ethephon (10μM), a prodrug of ethylene, and a non-chem. treated control were found to be 128 ± 19 and 58 ± 16°, resp. Compound II also exhibited potent activity on reducing stem elongation. The hypocotyl length of Arabidopsis seedlings treated with compound II (10μM) was found to be 0.25 ± 0.02 cm, while those of ethephon-treated (10μM) and treated controls were found to be 0.69 ± 0.06 and 1.15 ± 0.01 cm, resp. Compound II displayed potency inhibiting the root growth of Arabidopsis seedlings similar to that of ethephon.

Journal of Pesticide Science (Tokyo, Japan) published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Name: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

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

Zhang, Jian published the artcilePurine Nucleoside Derivatives Containing a Sulfa Ethylamine Moiety: Design, Synthesis, Antiviral Activity, and Mechanism, Quality Control of 32333-53-2, the publication is Journal of Agricultural and Food Chemistry (2021), 69(20), 5575-5582, database is CAplus and MEDLINE.

To find efficient and broad-spectrum viral agents, a series of purine nucleoside derivatives containing sulfa ethylamine moieties was designed and synthesized, and their antiviral activities against tobacco mosaic virus (TMV), cucumber mosaic virus (CMV), and potato virus Y (PVY) were evaluated. Some target compounds displayed good antiviral activities. Among them, compound I showed excellent protective activity against CMV and PVY with 50% effective concentration values (EC₅₀) of 137 and 209μg/mL, resp., which were better than that of the control agent ningnanmycin (508 and 431μg/mL). Moreover, the EC₅₀ value of compound I for the inactivating activity against TMV was 48μg/mL, which was better than that of ningnanmycin (88μg/mL). In addition, compound I not only destroyed the structure of the TMV virus but also had a good interaction with the coat protein of the TMV virus. Therefore, compound I may further destroy the structure of the virus by binding to the coat protein of the TMV virus, thereby weakening the infectivity of the virus.

Journal of Agricultural and Food Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C11H24O3, Quality Control of 32333-53-2.

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

Ramsbeck, Daniel published the artcileFirst insight into structure-activity relationships of selective meprin β inhibitors, SDS of cas: 32333-53-2, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(11), 2428-2431, database is CAplus and MEDLINE.

The astacin proteases meprin α and β are emerging drug targets for treatment of disorders such as kidney failure, fibrosis or inflammatory bowel disease. However, there are only few inhibitors of both proteases reported to date. Starting from NNGH as lead structure, a detailed elaboration of the structure-activity relationship of meprin β inhibitors was performed, leading to compounds with activities in the lower nanomolar range. Considering the preference of meprin β for acidic residues in the P1′ position, the compounds were optimized. Acidic modifications induced potent inhibition and >100-fold selectivity over other structurally related metalloproteases such as MMP-2 or ADAM10.

Bioorganic & Medicinal Chemistry Letters published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, SDS of cas: 32333-53-2.

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

Wang, Gren Z. published the artcileCCR2 receptor antagonists: Optimization of biaryl sulfonamides to increase activity in whole blood, Synthetic Route of 32333-53-2, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(24), 7291-7294, database is CAplus and MEDLINE.

A series of N,S-diarylsulfonamides was identified as hCCR2 receptor antagonists but suffered from high plasma protein binding resulting in a >100 fold shift in activity in a functional GTPγS assay run in tandem in the presence and absence of human serum albumin. Introduction of an aryl amide with ethylenediamine linker led to compounds with reduced shifts and improved activity in whole blood.

Bioorganic & Medicinal Chemistry Letters published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C9H20Cl2Si, Synthetic Route of 32333-53-2.

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

Toja, E. published the artcileAmnesia-reversal activity of a series of 5-alkoxy-1-arylsulfonyl-2-pyrrolidinones, Application In Synthesis of 32333-53-2, the publication is European Journal of Medicinal Chemistry (1991), 26(4), 403-13, database is CAplus.

A series of 5-alkoxy-1-arylsulfonyl-2-pyrrolidinones were prepared by condensation of arylsulfonyl chlorides with 5-alkoxy-2-pyrrolidinones. Most compounds reversed electroconvulsive shock-induced amnesia in mice, showing the typical inverted U-shaped dose-response curve. The results for 58 compounds indicate that the potency is maximum when there is a 5-ethoxy group and progressively declines as the ether alkyl chain is either elongated or shortened. Substitution on the Ph ring or its replacement with heterocyclic rings or its hydrogenation decreases the activity. The most promising compounds, with anti-amnesic properties superior in many respects (greater potency, greater efficacy and broader active dose-range) to those of piracetam and antiracetam were further evaluated for reversing scopolamine-induced amnesia and for their antihypoxic activity. 5-Ethoxy-1-phenylsulfonyl-2-pyrrolidinone and 5-(1-methylethoxy)-1-[3-(trifluoromethyl)phenylsulfonyl]-2-pyrrolidinone were selected for further evaluation because of their potent anti-amnesic and/or antihypoxic activity.

European Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C9H7NO2, Application In Synthesis of 32333-53-2.

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

Niculescu-Duvaz, Dan published the artcilePyridoimidazolones as Novel Potent Inhibitors of v-Raf Murine Sarcoma Viral Oncogene Homologue B1 (BRAF). [Erratum to document cited in CA150:472622], Recommanded Product: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Journal of Medicinal Chemistry (2009), 52(18), 5770, database is CAplus.

On page 2256, the authors have been notified by Plexxikon that the structure of PLX4032, published in Expert Opin. Ther. Targets 2007, 11, (12), 1587-1609 (Figure 4) in Figure 1, was incorrect and the correct one has not been released.

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Recommanded Product: 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

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

Niculescu-Duvaz, Dan published the artcilePyridoimidazolones as Novel Potent Inhibitors of v-Raf Murine Sarcoma Viral Oncogene Homologue B1 (BRAF), SDS of cas: 32333-53-2, the publication is Journal of Medicinal Chemistry (2009), 52(8), 2255-2264, database is CAplus and MEDLINE.

BRAF is a serine/threonine kinase that is mutated in a range of cancers, including 50-70% of melanomas, and has been validated as a therapeutic target. The authors have designed and synthesized mutant BRAF inhibitors containing pyridoimidazolone as a new hinge-binding scaffold. Compounds have been obtained which have low nanomolar potency for mutant BRAF (12 nM for compound I) and low micromolar cellular potency against a mutant BRAF melanoma cell line, WM266.4. The series benefits from very low metabolism, and pharmacokinetics (PK) that can be modulated by methylation of the NH groups of the imidazolone, resulting in compounds with fewer H-donors and a better PK profile. These compounds have great potential in the treatment of mutant BRAF melanomas.

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, SDS of cas: 32333-53-2.

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

Johnson, Sherida L. published the artcileStructure-activity relationship studies of a novel series of anthrax lethal factor inhibitors, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Bioorganic & Medicinal Chemistry (2009), 17(9), 3352-3368, database is CAplus and MEDLINE.

We report on the identification of a novel small mol. inhibitor of anthrax lethal factor using a high-throughput screening approach. Guided by mol. docking studies, we carried out structure-activity relationship (SAR) studies and evaluated activity and selectivity of most promising compounds in in vitro enzyme inhibition assays and cellular assays. Selected compounds were further analyzed for their in vitro ADME properties, which allowed us to select two compounds for further preliminary in vivo efficacy studies. The data provided represents the basis for further pharmacol. and medicinal chem. optimizations that could result in novel anti-anthrax therapies.

Bioorganic & Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Safety of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

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

Ortiz Zacarias, Natalia V. published the artcileDesign and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2, SDS of cas: 32333-53-2, the publication is Journal of Medicinal Chemistry (2021), 64(5), 2608-2621, database is CAplus and MEDLINE.

Covalently acting inhibitors constitute a large and growing fraction of approved small-mol. therapeutics as well as useful tools for a variety of in vitro and in vivo applications. Here, we aimed to develop a covalent antagonist of CC chemokine receptor 2 (CCR2), a class A GPCR that has been pursued as a therapeutic target in inflammation and immuno-oncol. Based on a known intracellularly binding CCR2 antagonist, several covalent derivatives were synthesized and characterized by radioligand binding and functional assays. These studies revealed compound 14 as an intracellular covalent ligand for CCR2. In silico modeling followed by site-directed mutagenesis confirmed that 14 forms a covalent bond with one of three proximal cysteine residues, which can be engaged interchangeably. To our knowledge, compound 14 represents the first covalent ligand reported for CCR2. Due to its unique properties, it may represent a promising tool for ongoing and future studies of CCR2 pharmacol.

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, SDS of cas: 32333-53-2.

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