56593-99-8

Upstream product

• 636-76-0 3-sulfamoylbenzoic acid 
• 68-12-2 N,N-dimethyl-formamide 
• 4025-64-3 3-Carboxybenzenesulfonyl chloride 

Downstream Products

• 59815-35-9 3'-sulfamoyl-diazoacetophenone 
• 59815-36-0 α-chloro-3-sulphamoylacetophenone 
• 712270-20-7 3-(aminosulfonyl)-N-{2'-[(4-fluorophenyl)amino]-4,4'-bipyridin-2-yl}benzamide 
• 220798-42-5 3-(hydroxymethyl)benzenesulfonamide 
• 1448009-59-3 methyl 2-(3-sulfamoylbenzamido)benzoate 
• 420831-33-0 2-(3-sulfamoylbenzamido)benzoic acid 

Relevant academic research and scientific papers

N-(sulfamoylbenzoyl)-l-proline derivatives as potential non-β-lactam esbl inhibitors: Structure-based lead identification, medicinal chemistry and synergistic antibacterial activities

Background: There is an urgent need to develop novel inhibitors against clinically widespread extended-spectrum β-lactamases (ESBLs) to meet the challenges of the ever-evolving threat of antibiotic resistances. Most existing ESBL inhibitors sharing a common chemical feature of β-lactam ring in their molecule, this structural characteristic makes them intrinsically susceptible to enzymatic breakdown by the resistance mechanisms employed by the bacteria. Objective: The aim of this study was to screen and discover novel lead compounds by using Lproline as initial scaffold to create a “non-sulfur, non-β-lactam” new chemotypes for potential ESBL inhibitors. Methods: Structure-based molecular docking and virtual screening were employed in the novel inhibitor generation process for lead compound screening and SAR analysis. Evaluation of the ESBL inhibitory activity of the lead compounds was performed in combination with three of the most susceptible antibiotics: ceftazidime, meropenem and ampicillin, against thirteen ESBL enzymes including four new CTX-M harboring strains and four KPC-2 producing species. Results: L-proline derived (S)-1-(2-sulfamoylbenzoyl)pyrrolidine-2-carboxylic acid (compound 6) as a “non-sulfur, non-β-lactam” and the most potential ESBL inhibitor was identified. Compound 6 possesses ideal anti-resistance activities by reducing MICs of ceftazidime, meropenem and ampicillin by 16-133, 32-133 and 67-267 fold respectiveily. The inhibitory mechanism of 6 with CTX-M, KPC-2 and penicillinase were proposed and probed with molecular docking analysis. Conclusion: Given that the simple proline derivative but promising synergistic antibacterial properties of compound 6 augers well for further investigations into its in vivo efficacy.

Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors

Many diseases are believed to be driven by pathological levels of reactive oxygen species (ROS) and oxidative stress has long been recognized as a driver for inflammatory disorders. Apoptosis signal-regulating kinase 1 (ASK1) has been reported to be activ

N-substituted phenyl-3-sulfonyl amino-benzamide compounds as well as preparation thereof and application thereof in anti-breast cancer activity

The invention discloses N-substituted phenyl-3-sulfonyl amino-benzamide compounds as well as preparation thereof and application thereof in anti-breast cancer activity. 3-sulfonyl amino-benzoic acid is used as a raw material; the compounds are prepared by

Structure optimization of 2-benzamidobenzoic acids as PqsD inhibitors for Pseudomonas aeruginosa infections and elucidation of binding mode by SPR, STD NMR, and molecular docking

Pseudomonas aeruginosa employs a characteristic pqs quorum sensing (QS) system that functions via the signal molecules PQS and its precursor HHQ. They control the production of a number of virulence factors and biofilm formation. Recently, we have shown that sulfonamide substituted 2-benzamidobenzoic acids, which are known FabH inhibitors, are also able to inhibit PqsD, the enzyme catalyzing the last and key step in the biosynthesis of HHQ. Here, we describe the further optimization and characterization of this class of compounds as PqsD inhibitors. Structural modifications showed that both the carboxylic acid ortho to the amide and 3′-sulfonamide are essential for binding. Introduction of substituents in the anthranilic part of the molecule resulted in compounds with IC50 values in the low micromolar range. Binding mode investigations by SPR with wild-type and mutated PqsD revealed that this compound class does not bind into the active center of PqsD but in the ACoA channel, preventing the substrate from accessing the active site. This binding mode was further confirmed by docking studies and STD NMR.

NOVEL PIPERIDINE DERIVATIVE

The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0 - 4, provided 3 ≤ m + n ≤ 8; X is nitrogen atom or a group of the formula: C-R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4 , R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.

Thiazolidine derivatives

The invention relates to thiazolidine derivatives having in 4-position a hydroxy group and a 3'-sulphamyl-phenyl substituent, in 2-position an imino group and in 1-position an aliphatic or cycloaliphatic substituent. Said thiazolidines have diuretic activity. The invention also relates to a process for the manufacture of said compounds.