110630-87-0

Upstream product

• 588679-10-1 ethyl 2-(4-bromo-2-chlorophenoxy)acetate 
• 77228-67-2 2-(4-bromo-2-chlorophenoxy) acetic acid 
• 1040308-89-1 (4-bromo-2-chloro-phenoxy)-acetic acid methyl ester 

Downstream Products

• 587841-69-8 2-(4-bromo-2-chlorophenoxy)-N-(4-sulfamoylphenylcarbamothioyl)acetamide 
• 1449004-30-1 N-(4-(N-benzoylsulfamoyl)phenylcarbamothioyl)-2-(4-bromo-2-chlorophenoxy) acetamide 
• 1449004-31-2 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-phenylacetylsulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-32-3 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(L-2-phenylglycyl)-sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-33-4 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-2-phenylglycyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-34-5 (S)-2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-2-(4-acetoxyphenyl)glycyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-35-6 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-tert-butoxycarbonyl-L-(2-phenyl)glycyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-36-7 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Lphenylalanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-37-8 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-L-3-(4-nitrophenyl)alanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-38-9 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Ltryptophanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-64-1 N-(4-(N-(L-leucyl)sulfamoyl)-phenylcarbamothioyl)-2-(4-bromo-2-chlorophenoxy) acetamide 
• 1449004-65-2 N-(4-(N-(N-carbobenzoxy-(L-leucyl))-sulfamoyl)phenylcarbamothioyl)-2-(4-bromo-2-chlorophenoxy)acetamide 
• 1449004-66-3 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-tert-butoxycarbonyl-Lleucyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-67-4 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Lisoleucyl)sulfamoyl)phenylcarbamothioyl)acetamide 

Relevant academic research and scientific papers

Design and synthesis of α-phenoxy-N-sulfonylphenyl acetamides as Trypanosoma brucei Leucyl-tRNA synthetase inhibitors

Human African trypanosomiasis (HAT), caused by the parasitic protozoa Trypanosoma brucei, is one of the fatal diseases in tropical areas and current medicines are insufficient. Thus, development of new drugs for HAT is urgently needed. Leucyl-tRNA synthetase (LeuRS), a recently clinically validated antimicrobial target, is an attractive target for development of antitrypanosomal drugs. In this work, we report a series of α-phenoxy-N-sulfonylphenyl acetamides as T. brucei LeuRS inhibitors. The most potent compound 28g showed an IC50 of 0.70 μM which was 250-fold more potent than the starting hit compound 1. The structure-activity relationship was also discussed. These acetamides provided a new scaffold and lead compounds for the further development of clinically useful antitrypanosomal agents.

Design and Synthesis of Novel 4-Hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one Derivatives for Use as Herbicides and Evaluation of Their Mode of Action

In order to develop a novel herbicide containing the β-triketone motif, a series of 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one derivatives were designed and synthesized. The bioassay results showed that compound II15 had good pre-emergent herbicidal activity even at a dosage of 187.5 g ha-1. Moreover, compound II15 showed a broader spectrum of weed control when compared with a commercial herbicide 2,4-dichlorophenoxyacetic acid (2,4-D), and displayed good crop safety to Triticum aestivum L. and Zea mays Linn. when applied at 375 g ha-1 under pre-emergence conditions, which indicated its great potential as a herbicide. More importantly, studying the molecular mode of action of compound II15 revealed that the novel triketone structure is a proherbicide of its corresponding phenoxyacetic acid auxin herbicide, which has a herbicidal mechanism similar to that of 2,4-D. The present work indicates that the 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one motif may be a potential lead structure for further development of novel auxin-type herbicides.

Cdc42 Inhibitor and Uses Thereof

Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demo

Discovery of N-(4-sulfamoylphenyl)thioureas as Trypanosoma brucei leucyl-tRNA synthetase inhibitors

Human African trypanosomiasis (HAT) is one of the most neglected diseases in the tropic regions, which is fatal if not treated in time. There is an urgent need for new therapeutics, especially those in new chemical classes. Leucyl-tRNA synthetase (LeuRS) has been paid much attention as a recently clinically validated antimicrobial target. Our group has previously reported T. brucei LeuRS (TbLeuRS) inhibitors, including benzoxaboroles targeting the editing site and pyrrolinones targeting the synthetic site. Here we report the discovery of N-(4-sulfamoylphenyl)thioureas as a new class of TbLeuRS inhibitors. The R1 and R2 groups, reminiscent of the leucyl and adenyl regions of aa-AMP and aa-AMS, were optimized to result in a significant 13-fold increase of inhibitory activity (compound 19, IC 50 = 13.7 μM). Aided by ligand-protein docking, the 1,3-substitution at the central phenyl ring was predicted and proved to give significantly improved activity (59, IC50 = 1.1 μM). This work provided a new scaffold for the exploration of novel inhibitors against TbLeuRS, which may become potential therapeutics for the treatment of HAT.