DPD-Inspired Discovery of Novel LsrK Kinase Inhibitors: An Opportunity To Fight Antimicrobial Resistance was written by Stotani, Silvia;Gatta, Viviana;Medarametla, Prasanthi;Padmanaban, Mohan;Karawajczyk, Anna;Giordanetto, Fabrizio;Tammela, Paivi;Laitinen, Tuomo;Poso, Antti;Tzalis, Dimitros;Collina, Simona. And the article was included in Journal of Medicinal Chemistry in 2019.Product Details of 1711-11-1 This article mentions the following:
Antibiotic resistance is posing a continuous threat to global public health and represents a huge burden for society as a whole. In the past decade, the interference with bacterial quorum sensing (QS) (i.e., cell-cell communication) mechanisms has extensively been investigated as a valid therapeutic approach in the pursuit of a next generation of antimicrobials. (S)-4,5-Dihydroxy-2,3-pentanedione, commonly known as (S)-DPD, a small signaling mol. that modulates QS in both Gram-neg. and Gram-pos. bacteria, is phosphorylated by LsrK, and the resulting phospho-DPD activates QS. We designed and prepared a small library of DPD derivatives, characterized by five different scaffolds, and evaluated their LsrK inhibition in the context of QS interference. SAR studies highlighted the pyrazole moiety as an essential structural element for LsrK inhibition. Particularly, four compounds were found to be micromolar LsrK inhibitors (IC50 ranging between 100 μM and 500 μM) encouraging further exploration of novel analogs as potential new antimicrobials. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1Product Details of 1711-11-1).
3-Cyanobenzoyl chloride (cas: 1711-11-1) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Product Details of 1711-11-1
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics