Category: 870778-91-9

Chen, Yiding published the artcileCopper(I)-catalyzed sulfonylative Suzuki-Miyaura cross-coupling, Name: (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, the publication is Chemical Science (2017), 8(4), 3249-3253, database is CAplus and MEDLINE.

By using a simple copper(I) catalyst a high yielding sulfonylative-Suzuki-Miyaura cross-coupling reaction was developed. The process provided a single step route to diaryl sulfones from the direct combination of arylboronic acids, sulfur dioxide and aryl iodides, and represents the first sulfonylative variant of a classic cross-coupling reaction. Sulfur dioxide was delivered from the surrogate reagent, DABSO. Variation of the reaction conditions allowed interruption of the sulfonylative-Suzuki coupling, resulted in the formation of a presumed Cu-sulfinate intermediate. These sulfinates was trapped as their sodium salts and treated with electrophiles to allow access to arylalkyl sulfones, β-hydroxyl sulfones, sulfonamides and sulfonyl fluorides.

Chemical Science published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, Name: (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid.

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

Kalcic, Filip published the artcilePolysubstituted Pyrimidines as mPGES-1 Inhibitors: Discovery of Potent Inhibitors of PGE₂ Production with Strong Anti-inflammatory Effects in Carrageenan-Induced Rat Paw Edema, SDS of cas: 870778-91-9, the publication is ChemMedChem (2020), 15(15), 1398-1407, database is CAplus and MEDLINE.

We report an extensive structure-activity relationship optimization of polysubstituted pyrimidines that led to the discovery of 5-butyl-4-(4-benzyloxyphenyl)-6-phenylpyrimidin-2-amine, and its difluorinated analog. These compounds are sub-micromolar inhibitors of PGE₂ production (IC₅₀ as low as 12 nM). In order to identify the mol. target of anti-inflammatory pyrimidines, we performed extensive studies including enzymic assays, homol. modeling and docking. The difluorinated analog simultaneously inhibits two key enzymes of the arachidonic acid cascade, namely mPGES-1 and COX-2, with mPGES-1 inhibition being the principal mechanism of action. Other pyrimidines studied are potent mPGES-1 inhibitors with no observed inhibition of COX-1/2 enzymes. Moreover, the two most potent compounds proved to be significantly effective in vivo in a model of acute inflammation, suppressing carrageenan-induced rat paw edema by 36 and 46%. The promising results of this study warrant further preclin. evaluation of selected anti-inflammatory candidates.

ChemMedChem published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, SDS of cas: 870778-91-9.

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

Giordano, Assunta published the artcileVirtual Fragment Screening Identification of a Quinoline-5,8-dicarboxylic Acid Derivative as a Selective JMJD3 Inhibitor, Quality Control of 870778-91-9, the publication is ChemMedChem (2018), 13(12), 1160-1164, database is CAplus and MEDLINE.

The quinoline-5,8 dicarboxylic acid scaffold has been identified by a fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, 3-(2,4-dimethoxypyrimidin-5-yl)quinoline-5,8-dicarboxylic acid (compound 3) shows low micromolar inhibitory activity against Jumonji domain-containing protein 3 (JMJD3). The exptl. evaluation of inhibitory activity against seven related isoforms of JMJD3 highlighted an unprecedented selectivity toward the biol. target of interest.

ChemMedChem published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, Quality Control of 870778-91-9.

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

Nuti, Elisa published the artcileSugar-Based Arylsulfonamide Carboxylates as Selective and Water-Soluble Matrix Metalloproteinase-12 Inhibitors, Application of (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, the publication is ChemMedChem (2016), 11(15), 1626-1637, database is CAplus and MEDLINE.

Matrix metalloproteinase-12 (MMP-12) can be considered an attractive target to study selective inhibitors useful in the development of new therapies for lung and cardiovascular diseases. .In this study, a new series of arylsulfonamide carboxylates, with increased hydrophilicity resulting from conjugation with a β-N-acetyl-D-glucosamine moiety, were designed and synthesized as MMP-12 selective inhibitors. Their inhibitory activity was evaluated on human MMPs by using the fluorimetric assay, and a crystallog. anal. was performed to characterize their binding mode. Among these glycoconjugates, a nanomolar MMP-12 inhibitor with improved water solubility, compound I was identified.

ChemMedChem published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, Application of (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid.

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

Nuti, Elisa published the artcileN-O-Isopropyl Sulfonamido-Based Hydroxamates: Design, Synthesis and Biological Evaluation of Selective Matrix Metalloproteinase-13 Inhibitors as Potential Therapeutic Agents for Osteoarthritis, Formula: C13H12BClO3, the publication is Journal of Medicinal Chemistry (2009), 52(15), 4757-4773, database is CAplus and MEDLINE.

The synthesis and in vitro evaluation of a new series of selective matrix metalloproteinase-13 (MMP-13) inhibitors possessing an arylsulfonamidic scaffold was reported. Among these potential inhibitors, I was discovered exhibiting nanomolar activity for MMP-13 and was highly selective for this enzyme compared to MMP-1, -14, and TACE. Compound I acted as a slow-binding inhibitor of MMP-13 and was demonstrated to be effective in an in vitro collagen assay and in a model of cartilage degradation Furthermore, a docking study was conducted for this compound in order to investigate its binding interactions with MMP-13 and the reasons for its selectivity toward MMP-13 vs. other MMPs.

Journal of Medicinal Chemistry published new progress about 870778-91-9. 870778-91-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (4-((4-Chlorobenzyl)oxy)phenyl)boronic acid, and the molecular formula is C13H12BClO3, Formula: C13H12BClO3.

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