Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae – Identification of LYS228 was written by Reck, Folkert;Bermingham, Alun;Blais, Johanne;Capka, Vladimir;Cariaga, Taryn;Casarez, Anthony;Colvin, Richard;Dean, Charles R.;Fekete, Alex;Gong, Wanben;Growcott, Ellie;Guo, Hongqiu;Jones, Adriana K.;Li, Cindy;Li, Fengxia;Lin, Xiaodong;Lindvall, Mika;Lopez, Sara;McKenney, David;Metzger, Louis;Moser, Heinz E.;Prathapam, Ramadevi;Rasper, Dita;Rudewicz, Patrick;Sethuraman, Vijay;Shen, Xiaoyu;Shaul, Jacob;Simmons, Robert L.;Tashiro, Kyuto;Tang, Dazhi;Tjandra, Meiliana;Turner, Nancy;Uehara, Tsuyoshi;Vitt, Charles;Whitebread, Steven;Yifru, Aregahegn;Zang, Xu;Zhu, Qingming. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2018.SDS of cas: 15186-48-8 This article mentions the following:
Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of MBLs confers resistance in Gram-neg. bacteria to all classes of β-lactam antibiotics, with the exception of monobactams, which are intrinsically stable to MBLs. However, existing first generation monobactam drugs like aztreonam have limited clin. utility against MBL-expressing strains because they are impacted by serine β-lactamases (SBLs), which are often co-expressed in clin. isolates. Here, we optimized novel monobactams for stability against SBLs, which led to the identification of LYS228 (compound 31). LYS228 is potent in the presence of all classes of β-lactamases and shows potent activity against carbapenem-resistant isolates of Enterobacteriaceae (CRE). In the experiment, the researchers used many compounds, for example, (R)-2,2-Dimethyl-1,3-dioxolane-4-carbaldehyde (cas: 15186-48-8SDS of cas: 15186-48-8).
(R)-2,2-Dimethyl-1,3-dioxolane-4-carbaldehyde (cas: 15186-48-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Although benzodioxole is not particularly important, many related compounds containing the methylenedioxyphenyl group are bioactive, and thus are found in pesticides and pharmaceuticals.SDS of cas: 15186-48-8
Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem