Category: 7079-48-3

Spicer, Julie A. published the artcileSubstituted arylsulphonamides as inhibitors of perforin-mediated lysis, Name: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is arylsulfonamide perforin mediated lysis inhibitor structure activity Immunosuppressive; Arylsulphonamide; Bioisostere; Immunosuppressant; Perforin; Perforin inhibitor.

The structure-activity relationships for a series of arylsulfonamide-based inhibitors of the pore-forming protein perforin have been explored. Perforin is a key component of the human immune response, however, inappropriate activity has also been implicated in certain auto-immune and therapy-induced conditions such as allograft rejection and graft vs. host disease. Since perforin is expressed exclusively by cells of the immune system, inhibition of this protein would be a highly selective strategy for the immunosuppressive treatment of these disorders. Compounds from this series were demonstrated to be potent inhibitors of the lytic action of both isolated recombinant perforin and perforin secreted by natural killer cells in vitro. Several potent and soluble examples were assessed for in vivo pharmacokinetic properties and found to be suitable for progression to an in vivo model of transplant rejection.

European Journal of Medicinal Chemistry published new progress about Autoimmune disease. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Name: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Jiang, Fei published the artcileDiscovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis, Related Products of chlorides-buliding-blocks, the main research area is preparation benzoindolone pyrrolo quinolinone derivative BET inhibitor gout.

The bromodomain and extra-terminal domain (BET) family of proteins are readers which specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein contains two highly homologous domains: the first bromodomain (BD1) and the second bromodomain (BD2). Pan-BET bromodomain inhibition is a potential therapy for various cancers and immune-inflammatory diseases, but only few reported inhibitors show selectivity within the BET family. Herein, we identified a series of benzo[cd]indol-2(1H)-ones and pyrrolo[4,3,2-de]quinolin-2(1H)-ones with good selectivity for BET BD1. Through structure-based optimization, highly active and selective compounds are ultimately obtained. The representative compounds are the first reported inhibitors with selectivity more than 100-fold for BRD4(1) over BRD4(2). Among them, we further show that 68 (LT052) mediates BRD4/NF-κB/NLRP3 signaling inflammatory pathways with comparable protein expression and significantly improves symptoms of gout arthritis in a rat model. Therefore, selective pharmacol. modulation of individual bromodomains could represent a strategy for the treatment of acute gouty arthritis.

Journal of Medicinal Chemistry published new progress about Bromodomain-containing protein BRD4 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Related Products of chlorides-buliding-blocks.

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

Nie, Li Fei published the artcileSynthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells, Quality Control of 7079-48-3, the main research area is thienopyrimidinone benzenesulfonamide preparation melanin synthesis activity.

A series of novel sulfonamide derivatives containing tricyclic thieno[2,3-d]pyrimidinones I (R = Ph, 4-FC6H4, 2-F3CC6H4, 3,5-Cl2C6H3, etc.) was synthesized and evaluated for melanin synthesis in murine B16 cells. All new compounds were characterized by 1H NMR, 13C NMR, IR and HRMS. Among them, 6 compounds demonstrated excellent activity than pos. control (8-methoxylpsoralen, 8-MOP) with more than 1.5-fold potency. Compound I (R = 3,5-Cl2C6H3) was the most potent one (658.3 ± 8.7%), exhibiting 5.0-fold stronger activity than 8-MOP (130.9 ± 8.6%). The compound I (R = 3,5-F2C6H3) increased melanin synthesis in murine B16 cells with a 4.35-fold potency as compared to 8-MOP. These compounds may serve as lead compounds for further drug discoveries for the treatment of vitiligo.

Research on Chemical Intermediates published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Quality Control of 7079-48-3.

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

Nie, Li Fei published the artcileDesign, synthesis, and toward a side-ring optimization of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones and their effect on melanin synthesis in murine B16 cells, Product Details of C7H6ClFO2S, the main research area is oxo tetrahydro pyrrolothienopyrimidinyl benzenesulfonamide preparation melanin synthesis activity; methyl oxo hexahydro thienopyrimidoazepinyl benzenesulfonamide preparation melanin synthesis activity.

The synthesis of 48 novel 3-sulfonylamides containing a tricyclic thieno[2,3-d]pyrimidin-4(3H)-one moiety, I [R1 = H, 3-F, 3-NO2, etc.; R2 = H, 4-Me, 5-Cl, etc.; n = 1,3], and their influence on melanin synthesis in murine B16 cells. All target sulfonylamides I were synthesized through key intermediate 3-nitro-thieno[2,3-d]pyrimidin-4(3H)-ones using three types of ipso-nitration reactions. In this case, the pyrido[1,2-a]- fragment of the thieno[2,3-d]pyrimidine moiety was converted to pyrrolo[1,2-a]- and azepino[1,2-a]- side-rings in order to evaluate the bioactivities of the synthesized derivatives for a structure activity-relationships point of view. The obtained results suggested that some of the selected compounds revealed a promising influence on melanin synthesis in murine B16 cells and may serve as lead compounds for further drug discovery and development.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Product Details of C7H6ClFO2S.

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

Gajera, Nilesh N. published the artcileSynthesis, characterization and biological screening of new spirochromanones, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is spirochromanone leucine benzenesulfonamide preparation antibacterial antifungal.

New spirochromanones I (R = substituted phenyl) based on N-[1-(6-bromo-4-oxo-3,4-dihydro-1’H-spiro[chromene-2,4′-piperidin]-1′-yl)-3-methyl-1-oxobutan-2-yl]benzenesulfonamides were synthesized by series of reactions, such as cyclization, deprotection, coupling, and condensation. The compounds were tested for their activity against fungi and pathogenic strains of bacteria. The compounds bearing F, cyano, and OCF3 groups at para position showed competitive antifungal activity, while the compounds carrying either a halo or Me substituent at ortho position showed significant antibacterial activity.

Journal of Chemical and Pharmaceutical Research published new progress about Antibacterial agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Yang, Peng-Yu published the artcileSolid-Phase Synthesis of Azidomethylene Inhibitors Targeting Cysteine Proteases, COA of Formula: C7H6ClFO2S, the main research area is azidomethylene library solid phase preparation inhibitor cysteine protease caspase.

An efficient strategy for the solid-phase synthesis of azidomethylene inhibitors targeting cysteine proteases is described. The method is highlighted by its compatibility with readily available building blocks, as well as its ability to accommodate different functional groups. A 249-member library has thus far been successfully synthesized, characterized, and screened against caspase-1, -3 and -7.

Organic Letters published new progress about Enzyme inhibitors. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, COA of Formula: C7H6ClFO2S.

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