15054-44-1

Upstream product

• 56-40-6 glycine 
• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 156840-00-5 2,4-dinitrophenyl 4-nitrobenzenesulfonate 

Downstream Products

• 83800-74-2 1-(4-Nitro-benzenesulfonyl)-2-thioxo-imidazolidin-4-one 
• 5616-30-8 2-(4-aminobenzenesulfonylamino)ethanoic acid 
• 1060662-36-3 methyl (2S)-6-(4-nitrobenzenesulfonyl)-2-(benzyloxymethyl)-3,6-diaza-4-oxohexanoate 
• 106148-57-6 N-(4-nitrophenylsulfonyl)glycinoyl chloride 
• 1431285-91-4 N₁-[(1S,2S,3E)-2-{[(1,1-dimethylethyl)(dimethyl)silyl] oxy}-4-phenyl-1-(2-propen-1-yl)-3-buten-1-yl]-N₂-[(4-nitrophenyl)sulfonyl]glycinamide 
• 109065-79-4 [4-(2-Benzyloxy-acetylamino)-benzenesulfonylamino]-acetic acid 
• 109065-78-3 [4-(2-Phenoxy-acetylamino)-benzenesulfonylamino]-acetic acid 
• 58960-90-0 N-[(4-{[(benzyloxy)carbonyl]amino}phenyl)sulfonyl]glycine 
• 109065-74-9 N-[[4-[(2-Phenylethyl)carbonylamino]phenyl]sulfonyl]glycine 
• 109065-77-2 N-phenyl-N'-[4-(N-glycinylsulfonyl)phenyl]thiourea 
• 109065-76-1 N-phenyl-N'-[4-(N-glycinylsulfonyl)phenyl]urea 
• 109065-73-8 N-[[4-(Phenylacetylamino)phenyl]sulfonyl]glycine 
• 109065-75-0 {4-[(E)-(3-Phenyl-acryloyl)amino]-benzenesulfonylamino}-acetic acid 
• 109065-69-2 BAPSG 

Relevant academic research and scientific papers

From a MMP2/CK2 multitarget approach to the identification of potent and selective MMP13 inhibitors

In this article, we describe our efforts in the search of MMP2/CK2 dual targeting inhibitors. We have followed a rational drug design approach based on our experience in the selective inhibition of these two enzymes. We have successfully obtained highly a

Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety

The reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis and antitrypanosomal activity of 24 new amide derivatives of 3-aminoquinoline, bearing substituted benzenesulphonamide. Nine of the new derivatives showed comparable antitrypanosomal activities at IC50 range of 1–6 nM (melarsoprol 5 nM). Compound 11n and 11v are more promising antitrypanosomal agents with IC50 1.0 nM than the rest of the reported derivatives. The novel compounds showed satisfactory predicted physico-chemical properties including oral bioavailability, permeability and transport properties.

Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies

Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of t

Synthesis, characterization and anthelmintic activity evaluation of pyrimidine derivatives bearing carboxamide and sulphonamide moieties

Pyrimidines, sulphonamides and carboxamides have shown a large number of pharmacological properties against different types of diseases including helminthiasis. Seventeen new pyrimidine derivatives bearing sulphonamide and carboxamide were synthesized and

Synthesis, characterization, molecular docking and in?vitro antimalarial properties of new carboxamides bearing sulphonamide

Sulphonamides and carboxamides have shown large number of pharmacological properties against different types of diseases among which is malaria. Twenty four new carboxamide derivatives bearing benzenesulphonamoyl alkanamides were synthesized and investigated for their in silico and in?vitro antimalarial and antioxidant properties. The substituted benzenesulphonyl chlorides (1a-c) were treated with various amino acids (2a-h) to obtain the benzenesulphonamoyl alkanamides (3a-x) which were subsequently treated with benzoyl chloride to obtain the N-benzoylated derivatives (5a-f, i-n and q-v). Further reactions of the N-benzoylated derivatives or proline derivatives with 4-aminoacetophenone (6) using boric acid as a catalyst gave the sulphonamide carboxamide derivatives (7a-x) in excellent yields. The in?vitro antimalarial studies showed that all synthesized compounds had antimalarial property. Compound 7k, 7c, 7l, 7s, and 7j had mean MIC value of 0.02, 0.03, 0.05, 0.06 and 0.08?μM respectively comparable with chloroquine 0.06?μM. Compound 7c was the most potent antioxidant agent with IC50 value of 0.045?mM comparable with 0.34?mM for ascorbic acid. In addition to the successful synthesis of the target molecules using boric acid catalysis, the compounds were found to have antimalarial and antioxidant activities comparable with known antimalarial and antioxidant drugs. The class of compounds reported herein have the potential of reducing oxidative stress arising from malaria parasite and chemotherapeutic agent used in the treatment of malaria.

New carboxamide derivatives bearing benzenesulphonamide as a selective COX-II inhibitor: Design, synthesis and structure-activity relationship

Sixteen new carboxamide derivatives bearing substituted benzenesulphonamide moiety (7a-p) were synthesized by boric acid mediated amidation of appropriate benzenesulphonamide with 2-amino-4-picoline and tested for anti-inflammatory activity. One compound 7c showed more potent anti-inflammatory activity than celecoxib at 3 h in carrageenan-induced rat paw edema bioassay. Compounds 7g and 7k also showed good anti-inflammatory activity comparable to celecoxib. Compound 7c appeared selectivity index (COX-2/COX-1) better than celecoxib. Compound 7k appeared selectivity index (COX-2/COX-1) a little higher than the half of celecoxib while compound 7g is non-selective for COX-2. The LD50 of compounds 7c, 7g and 7k were comparable to celecoxib.

Imidazole [2, 1-b] thiazole derivative as well as preparation method and application thereof

The invention belongs to the field of chemical pharmaceuticals, and particularly relates to an imidazole [2, 1-b] thiazole derivative as well as a preparation method and an application thereof. The structure of the imidazole [2, 1-b] thiazole derivative i

As the NS4B inhibitor benzofuran analogs (by machine translation)

The present invention discloses a kind of as NS4B benzofuran analogue inhibitors, in particular to the formula (I) below or a pharmaceutically acceptable salt thereof. (by machine translation)

Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors

The identification of a series of sulfonyl-amino-acetamides as BACE-1 (β-secretase) inhibitors for the treatment of Alzheimer's disease is reported. The derivatives were designed based on the docking simulation study, synthesized and assessed for BACE-1 inhibition in vitro. The designed ligands revealed desired binding interactions with the catalytic aspartate dyad and occupance of S1 and S2′ active site regions. These in silico results correlated well with in vitro activity. Out of 33 compounds synthesized, 12 compounds showed significant inhibition at 10 μM concentration. The most active compound 2.17S had IC50 of 7.90 μM against BACE-1, which was concomitant with results of in silico docking study.

Discovery of imidazo[2,1- b ]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents

The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16