63233-85-2Relevant academic research and scientific papers
N-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting Pseudomonas aeruginosa Elastase and Clostridium Collagenases
Konstantinovi?, Jelena,Yahiaoui, Samir,Alhayek, Alaa,Haupenthal, J?rg,Sch?nauer, Esther,Andreas, Anastasia,Kany, Andreas M.,Müller, Rolf,Koehnke, Jesko,Berger, Fabian K.,Bischoff, Markus,Hartmann, Rolf W.,Brandstetter, Hans,Hirsch, Anna K. H.
supporting information, p. 8359 - 8368 (2020/09/16)
In light of the global antimicrobial-resistance crisis, there is an urgent need for novel bacterial targets and antibiotics with novel modes of action. It has been shown that Pseudomonas aeruginosa elastase (LasB) and Clostridium histolyticum (Hathewaya histolytica) collagenase (ColH) play a significant role in the infection process and thereby represent promising antivirulence targets. Here, we report novel N-Aryl-3-mercaptosuccinimide inhibitors that target both LasB and ColH, displaying potent activities in vitro and high selectivity for the bacterial over human metalloproteases. Additionally, the inhibitors demonstrate no signs of cytotoxicity against selected human cell lines and in a zebrafish embryo toxicity model. Furthermore, the most active ColH inhibitor shows a significant reduction of collagen degradation in an ex vivo pig-skin model.
Synthesis of cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) and evaluation of their antifungal potential
Stiz, Dorimar,Corrêa, Rogério,D'Auria, Felicia D.,Simonetti, Giovanna,Cechinel-Filho, Valdir
, p. 647 - 654 (2016/10/18)
Background: This paper describes the synthesis of three different subfamilies of cyclic imides: methylphtalimides, carboxyl acid phtalimides and itaconimides. Methods: Fifteen compounds (five of each sub-family) were obtained by the reaction of appropriat
SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME DERIVATIVES RELATED TO 2-METHYLENEBUTANEDIOIC ACID
Veverka, Miroslav,Kralovicova, Eva
, p. 2731 - 2737 (2007/10/02)
Nucleophilic reactions of methyl 3-chloroformyl-3-butenoate with N-substituted anilines and substituted phenols, and also preparation of 2-methylenebutanedioic acid monoanilides and their dehydration to the corresponding N-arylimides are described.
