74426-50-9

Upstream product

• 90536-66-6 4-(methylsulfonyl)phenylacetic acid 

Downstream Products

• 479680-02-9 N-methyl-N-(2-hydroxy-phenyl)ethyl-4-methylsulfonylphenacetamide 
• 374725-45-8 (4-methanesulfonyl-phenyl)-acetic acid amide 
• 178614-26-1 2-(4-fluorophenyl)-3-[4-(methylsulfonyl)phenyl]-1H-indole 
• 346413-00-1 1-(4-ethoxyphenyl)-2-[4-(methylsulfonyl)phenyl]ethanone 
• 1380646-39-8 (S)-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionic acid 
• 1380646-38-7 (S)-4-benzyl-3-[(S)-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionyl]oxazolidin-2-one 
• 1380645-86-2 (S)-N-Benzooxazol-2-yl-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionamide 
• 1380646-37-6 (S)-4-Benzyl-3-[(R)-2-(4-methanesulfonyl-phenyl)-3-o-tolyl-propionyl]-oxazolidin-2-one 
• 1380646-36-5 (S)-4-benzyl-3-[2-(4-methanesulfonyl-phenyl)-acetyl]-oxazolidin-2-one 
• 919754-93-1 diethyl 2-(2-(4-(methylsulfonyl)phenyl)acetamido)-4,5-dihydrothieno[2,3-c]pyridine-3,6(7H)-dicarboxylate 

Relevant academic research and scientific papers

Thiophene inhibitors of PDE4: Crystal structures show a second binding mode at the catalytic domain of PDE4D2

PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.

Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor

Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.

INHIBITION OF ENZYMES

Compounds of formula (I) are inhibitors of neutrophil elastase wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I).

2,3-Diaryl-substituted indole based COX-2 inhibitors as leads for imaging tracer development

A series of 2,3-diaryl-substituted indoles containing a fluorine or methoxy group was synthesized via Fischer indole synthesis, McMurry cyclization, or Bischler-Moehlau reaction to identify potential leads for positron emission tomography (PET) radiotracer development as well as for optical imaging. All 2,3-diaryl-substituted indoles possess autofluorescent properties with an emission maximum in a range of 443-492 nm, which is acceptable for biological studies in vitro and, in part, in vivo. The molecular structure of compounds 3a and 3j was confirmed by X-ray crystal structure analysis. COX inhibitory activity was evaluated by a fluorescence-based and enzyme immunoassay-based assay. Redox activity of all target compounds was also determined. All synthesized 2,3-diaryl-substituted indoles are inhibitors of COX-2 enzyme in the low micromolar range. Compounds 3e, 3f, 3g and 3m displayed a 30-40% inhibition of COX-2 at 0.1 μM concentration while compounds 3f and 3g also exhibited COX-1 inhibitory activity. Various compounds like 3g showed substantial antioxidative potential (RDIENE = 2.85, RHAVA = 1.98), an effect that was most measurable with methoxy-substituted compounds. With respect to PET radiotracer synthesis, OMe-containing compound 3j was selected as a promising candidate for carbon-11 labeling, and F-containing compound 3m as a lead for the development of a fluorine-18 labeled derivative. the Partner Organisations 2014.

A new class of "electro-acid/base"-induced reversible methyl ketone colour switches

Methyl ketone has been designed as a switching unit for electrically addressable molecular colour switches. A newly proposed mechanism of "electro-acid/base" (radical ions)-induced intermolecular proton transfer for the colour switch is proven clearly by cyclic voltammetry (CV), X-ray photoelectron spectroscopy (XPS), infrared spectroscopy (IR) and in situ UV-Vis spectroscopy. A dramatic spectral absorption shift (about 291 nm) is observed during the switching, and blue, yellow and green colours are obtained by adjusting the substituents on the methyl ketone-bridged unit. The in situ "electro-acid/base" is far more convenient than the conventional chemical stimulus of acids or bases for the manipulation of the molecular switching properties. This new switching method and molecular structure manipulation will inspire and accelerate the further development of broad switching materials and applications in ultrathin flexible displays, etc.

Amido Compounds

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof

The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associ

Sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones, preparation method, and medical use thereof

The invention relates to sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones compounds having formula (I) wherein R1 is selected from the group consisting of 4-methylsulfonyl, 4-aminosulfonyl, hydrogen, 2-, 3-, or 4-halogen, C1-C6

Sulfonyl-containing 2,3-diarylindole compounds, methods for making same, and methods of use thereof

The present invention relates to sulfonyl-containing 2,3-diarylindole, especially to new compounds of general Formula, to a preparation method for their preparation, to pharmaceutical compositions containing said compound, and to the medical use thereof in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).

Discovery of 2-phenyl-3-sulfonylphenyl-indole derivatives as a new class of selective COX-2 inhibitors

2-Sulfonylphenyl-3-phenyl-indole derivatives have been reported to be highly potent and selective COX-2 inhibitors previously. In this paper, the regio-isomeric analogues-2-phenyl-3-sulfonylphenyl-indoles were identified as potent and selective COX-2 inhi