Category: 97-09-6

On April 25, 2018, Gur, Zehra Tugce; Caliskan, Burcu; Garscha, UIrike; Olgac, Abdurrahman; Schubert, Ulrich S.; Gerstmeier, Jana; Werz, Oliver; Banoglu, Erden published an article.Formula: C6H5ClN2O4S The title of the article was Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7. And the article contained the following:

Leukotrienes (LTs) and prostaglandin (PG)E2 are enzymically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, the authors report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal prostaglandin E2 synthase (mPGES)-1 in LT and PGE2 biosynthesis, based on the previously identified selective FLAP inhibitor BRP-7 (8, IC50 = 0.31 μM). C -substitution of the benzimidazole ring of BRP-7 by carboxylic acid and its bioisosteres provided compounds, exemplified by 57 (5-{1-[(2-chlorophenyl)methyl]-2-{1-[4-(2-methylpropyl)phenyl]ethyl}-1H-benzimidazol-5-yl}-2,3-dihydro-1,3,4-oxadiazole-2-thione) that potently suppress LT formation (IC50 = 0.05 μM) by targeting FLAP along with inhibition of mPGES-1 (IC50 = 0.42 μM). Besides FLAP, also 5-lipoxygenase (5-LO) and LTC4 synthase activities were inhibited by 57, albeit with lower potency (IC50 = 0.6 and 6.2 μM) than FLAP. Docking studies and mol. dynamic simulations with FLAP, mPGES-1 and 5-LO provide valuable insights into potential binding interactions of the inhibitors with their targets. Together, these novel benzimidazole derivatives may possess potential as leads for development of effective anti-inflammatory drugs with multi-target properties for dually inhibiting LT and PGE2 production The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Formula: C6H5ClN2O4S

The Article related to multitarget inhibitor leukotriene prostaglandin e2 flap brp7 analog preparation, 5-lipoxygenase, 5-lipoxygenase-activating protein, benzimidazole, inflammation, leukotriene, microsomal prostaglandin e(2) synthase-1 and other aspects.Formula: C6H5ClN2O4S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kakeya, Nobuharu; Yata, Noboru; Kamada, Akira; Aoki, Masaru published an article in 1970, the title of the article was Biological activities of drugs. IX. Structure-activity relation of sulfonamide carbonic anhydrase inhibitors. 4.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide And the article contains the following content:

Hansch-Fujita’s equation has been applied to an anal. of the natriuretic activity of sulfonamide carbonic anhydrase inhibitors using π and πc as hydrophobic parameters, and σ, ΔpKa, Δppm and Δfr as electronic parameters. Sixteen benzenesulfonamide derivatives were satisfactorily applied to the structure-activity anal. of heterocyclic sulfonamides. It was concluded that a strong natriuretic activity was observed for sulfonamides which had an optimal hydrophobicity and low electronegativity at the sulfamoyl group or a strong inhibitory activity against carbonic anhydrase. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to structure activity sulfonamides antienzymic, activity structure sulfonamides antienzymic, sulfonamides antienzymic structure activity, antienzymic sulfonamides structure activity, carbonic anhydrase inhibitor structure and other aspects.Application In Synthesis of 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 1, 2020, Liu, Lulu; Liu, Renshuai; Yang, Xinying; Hou, Xuben; Fang, Hao published an article.Application of 97-09-6 The title of the article was Design, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors. And the article contained the following:

The upregulation of the protein myeloid cell leukemia-1 (Mcl-1) is closely associated with various human cancers, which can result in the evasion of apoptosis and a low survival rate. Therefore, developing Mcl-1 inhibitors has become a promising paradigm for cancer therapy. Herein, we designed and synthesized a novel series of tyrosine derivatives, among which compounds (I) (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) exhibited very high binding affinity to Mcl-1 with Ki values of 0.18, 0.27 and 0.23μM, resp. Interestingly, compound I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1) showed not only potent activity against Mcl-1 but also considerable selectivity over Bcl-2 and Bcl-xL, which was rationalized by mol. docking and fragment-centric topog. mapping (FCTM). It is worth noting that compounds I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) displayed potent antiproliferative activity against several cancer cell lines and could induce apoptosis of KM3 and HepG2 cells in a dose-dependent manner. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application of 97-09-6

The Article related to peptidomimetic tyrosine synthesis drug design apoptosis, mol docking mcl1 inhibitor peptidomimetic, tyrosine methyl ester bromoalkane condensation benzenesulfonamide amidation coupling, apoptosis, cancer, mcl-1 inhibitors, tyrosine derivatives and other aspects.Application of 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On February 28, 2018, Sapegin, Alexander; Kalinin, Stanislav; Angeli, Andrea; Supuran, Claudiu T.; Krasavin, Mikhail published an article.Recommanded Product: 97-09-6 The title of the article was Unprotected primary sulfonamide group facilitates ring-forming cascade en route to polycyclic [1,4]oxazepine-based carbonic anhydrase inhibitors. And the article contained the following:

4-Chloro-3-nitrobenzenesulfonamide reacted cleanly at room-temperature with a range of bis-electrophilic phenols bearing an NH-acidic functionality (secondary carboxamide or pyrazole) in the ortho-position. This produced a novel class of [1,4]oxazepine-based primary sulfonamides which exhibited strong inhibition of therapeutically relevant human carbonic anhydrases. 2-Chloronitrobenzene did not enter a similar cyclocondensation process, even under prolonged heating. Thus, the primary sulfonamide functionality plays a dual role by enabling the [1,4]oxazepine ring construction and acting as a enzyme prosthetic zinc-binding group when the resulting [1,4]oxazepine sulfonamides are employed as carbonic anhydrase inhibitors. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 97-09-6

The Article related to oxazepine primary sulfonamide preparation human carbonic anhydrase inhibitor, carbonic anhydrase inhibitors, electron-withdrawing group, isoform-selectivity, nucleophilic aromatic substitution, primary sulfonamide, reactivity-matched substrates, smiles rearrangement and other aspects.Recommanded Product: 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On October 31, 1991, Shepard, Kenneth L.; Graham, Samuel L.; Hudcosky, Ronald J.; Michelson, Stuart R.; Scholz, Thomas H.; Schwam, Harvey; Smith, Anthony M.; Sondey, John M.; Strohmaier, Kim M. published an article.Name: 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides. And the article contained the following:

For several decades a goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. (Hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides I [R = (CH2)nOH, CH2CH(OH)CH2OH, CH2CH2CMe2OH, etc., n = 2-5; R1 = H, Cl, F, NO2, CO2H, CO2Me, NH2; X = S, SO2] and II [R2 = (CH2)nOH, (CH2)mCO2Me, (CH2)3O2CCH2OMe, (CH2)3O2CCH2CHMe2, (CH2)3NHCH2CHMe2, X = S, SO2, n = 2-4, m = 2, 3] were prepared and examined for carbonic anhydrase inhibitory activity. Thus, condensation of 2-mercaptoethanol with (bromophenylsulfonyl)formamidine III gave I [R = (CH2)2OH, R1 = H, X = S]. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the α-chymotrypsinized rabbit model of ocular hypertension after topical instillation. The inhibitory potency could be increased by converting a sulfide to the sulfone. Adding an extra methylene into the 4-substituent of benzene derivatives increases the inhibitory potency slightly more than oxidation of the sulfide. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Name: 3-Nitro-4-chlorobenzenesulfonamide

The Article related to hydroxyalkylsulfonylbenzenesulfonamide preparation carbonic anhydrase inhibitor, hydroxyalkylsulfonylthiophenesulfonamide preparation carbonic anhydrase inhibitor, carbonic anhydrase inhibitor hydroxyalkylsulfonylbenzenesulfonamide hydroxyalkylsulfonylthiophenesulfonamide, glaucoma treatment alkylsulfonylbenzenesulfonamide thiophenesulfonamide and other aspects.Name: 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 1, 2015, Wan, Yichao; Wu, Shaolei; Xiao, Guizhi; Liu, Tingting; Hou, Xuben; Chen, Chen; Guan, Peng; Yang, Xinying; Fang, Hao published an article.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors. And the article contained the following:

The B-cell lymphoma-2 (Bcl-2) protein is a promising target for cancer therapy. In the present study, a series of 2-thioxo-4-thiazolidinone derivatives were designed and synthesized as Bcl-2 inhibitors. Most of them possessed decent inhibitory activity for anti-apoptotic Bcl-2 proteins. Among them, compound I has similar growth inhibition towards K562 compared to (R)-Gossypol. In addition, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with a Ki value of 74 nM. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to thioxothiazolidinone derivative preparation preliminary bioactivity bcl2 inhibitor, oxothiazolidinethione derivative preparation preliminary bioactivity bcl2 inhibitor, cancer therapy growth inhibition thioxothiazolidinone derivative, 2-thioxo-4-thiazolidinone, anti-tumor, bcl-2, inhibitors and other aspects.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 26, 1998, Potrzebowski, Marek J.; Michalska, Maria; Koziol, Anna E.; Kazmierski, Slawomir; Lis, Tadeusz; Pluskowski, January; Ciesielski, Wlodzimierz published an article.Related Products of 97-09-6 The title of the article was Structural Implications of C-H···S Contacts in Organophosphorus Compounds. Studies of 1,6-Anhydro-2-O-tosyl-4-S-(5,5-dimethyl-2-thioxa-1,3,2-dioxaphosphorinan-2-yl)-β-D-glucopyranose by X-ray and Solid-State NMR Methods. And the article contained the following:

1,6-Anhydro-2-O-tosyl-4-S-(5,5-dimethyl-2-thioxa-1,3,2-dioxaphosphorinan-2-yl)-β-D-glucopyranose (1, C18H25O8PS3), crystallized from polar and/or nonpolar solvents, forms different modifications in the solid phase. Crystal structures of 1 (obtained from a methanol solution) and its 2-propanol solvate (1a) were established by X-ray structure anal. at low temperature One-component crystal 1 is orthorhombic, space group P212121, with a = 7.483(4) Å, b = 11.156 (6) Å, c = 27.11(2) Å, V = 2263 (2) Å3, Z = 4, and Dc = 1.457 g cm-3. The crystal of 1a is an inclusion structure containing mols. of 1 and 2-propanol in the ratio 1/1; crystals are triclinic, space group P1, with a = 9.637(6) Å, b = 9.709(6) Å, c = 8.865(8) Å, α = 110.27(5)°, β = 106.33(5)°, γ = 108.70(6)°, V = 661.3(8) Å3, Z = 1, and Dc = 1.398 g cm-3. Intermol. hydrogen bonds (O-H···O, C-H···O in 1; O-H···O, O-H···S in 1a) are present along with the C-H···S:P intermol. interactions. The solid-state structures were studied by the NMR spectroscopy. The presence of toluene-d8 in the crystal lattice of inclusion complex was confirmed by 2H NMR spectroscopy. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Related Products of 97-09-6

The Article related to toluene inclusion anhydrotosylthioxadioxaphosphorinanyl glucopyranose crystal structure, propanol solvate anhydrotosylthioxadioxaphosphorinanyl glucopyranose crystal structure, intermol hydrogen bond anhydrotosylthioxadioxaphosphorinanyl glucopyranose nmr, mol crystal structure anhydrotosylthioxadioxaphosphorinanyl glucopyranose and other aspects.Related Products of 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics