35331-31-8

Upstream product

• 2564-05-8 2-chloro-N-(3-chlorophenyl)acetamide 
• 108-42-9 3-chloro-aniline 
• 68-11-1 mercaptoacetic acid 

Downstream Products

• 222403-73-8 N,N'-bis(3-chlorophenyl)-3,6-dithiaoctanediamide 
• 1281988-16-6 2-(3-chlorophenylamino)-2-oxoethyl 3-chlorobenzo[b]thiophene-2-carbothioate 
• 1281988-41-7 2-(3-chlorophenylamino)-2-oxoethyl 3,6-dichlorobenzo[b]thiophene-2-carbothioate 
• 132389-29-8 N-(3-Chlorophenyl)-3-hydroxythieno[2,3-b]pyridine-2-carboxamide 

Relevant academic research and scientific papers

N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB fromPseudomonas aeruginosa

Increasing antimicrobial resistance is evolving to be one of the major threats to public health. To reduce the selection pressure and thus to avoid a fast development of resistance, novel approaches aim to target bacterial virulence instead of growth. Another strategy is to restore the activity of antibiotics already in clinical use. This can be achieved by the inhibition of resistance factors such as metallo-β-lactamases (MBLs). Since MBLs can cleave almost all β-lactam antibiotics, including the “last resort” carbapenems, their inhibition is of utmost importance. Here, we report on the synthesis andin vitroevaluation ofN-aryl mercaptoacetamides as inhibitors of both clinically relevant MBLs and the virulence factor LasB fromPseudomonas aeruginosa. All testedN-aryl mercaptoacetamides showed low micromolar to submicromolar activities on the tested enzymes IMP-7, NDM-1 and VIM-1. The two most promising compounds were further examined in NDM-1 expressingKlebsiella pneumoniaeisolates, where they restored the full activity of imipenem. Together with their LasB-inhibitory activity in the micromolar range, this class of compounds can now serve as a starting point for a multi-target inhibitor approach against both bacterial resistance and virulence, which is unprecedented in antibacterial drug discovery.

Synthesis and cytotoxicity of thieno[2,3-b]pyridine and furo[2,3-b]pyridine derivatives

Forty seven thieno[2,3-b]pyridines-2-carboxamides, furo[2,3-b]pyridines-2-carboxamides and tetrahydrothieno[2,3-b]quinolones-2-carboxamides derivatives were synthesized and tested for their antiproliferative activity against the NCI-60 cell lines. The 5-keto-tetrahydrothieno[2,3-b]quinolones-2-carboxamides (series 17) were found to have the greatest activity, with the compound containing a 3-methoxyphenylcarboxamide (compound 17d) being the most active, with GI50values in the low nanomolar range against a range of cell lines, in particular the melanoma cell line MDA-MD-435 (GI50- 23 nM) and the breast cancer cell line MDA-MB-468 (GI50- 46 nM). Molecular modelling of series 17 against phosphoinositide specific-phospholipase C reveals that the side chains of the amino acids His356, Glu341, Arg549 and Lys438 are involved in hydrogen bonding with the ligands as well as a lipophilic pocket is occupied by the phenyl carboxamide moiety.

Designer ligands. Part 2. Synthesis of novel, dithiadicarboxamide ligands

Novel, sulfur-containing diamide ligands have been synthesised, and preliminary complexation studies indicate their selectivity for palladium (II) over copper (II), nickel (II) and cobalt (II).