Product Details of 194726-40-4On May 10, 2018 ,《Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using β-Lactamase Inhibitors and β-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234》 appeared in Journal of Medicinal Chemistry. The author of the article were Papp-Wallace, Krisztina M.; Nguyen, Nhu Q.; Jacobs, Michael R.; Bethel, Christopher R.; Barnes, Melissa D.; Kumar, Vijay; Bajaksouzian, Saralee; Rudin, Susan D.; Rather, Philip N.; Bhavsar, Satish; Ravikumar, Tadiparthi; Deshpande, Prasad K.; Patil, Vijay; Yeole, Ravindra; Bhagwat, Sachin S.; Patel, Mahesh V.; van den Akker, Focco; Bonomo, Robert A.. The article conveys some information:
Limited treatment options exist to combat infections caused by multidrug-resistant (MDR) Gram-neg. bacteria possessing broad-spectrum β-lactamases. The design of novel β-lactamase inhibitors is of paramount importance. Here, three novel diazabicyclooctanes (DBOs), WCK 5153, zidebactam (WCK 5107), and WCK 4234 (compounds 1-3, resp.), were synthesized and biochem. characterized against clin. important bacteria. Compound 3 inhibited class A, C, and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. Compounds 1 and 2 acylated class A and C β-lactamses rapidly but not the tested OXAs. Compounds 1-3 formed highly stable acyl-complexes as demonstrated by mass spectrometry. Crystallog. revealed that 1-3 complexed with KPC-2 adopted a “”chair conformation”” with the sulfate occupying the carboxylate binding region. The cefepime-2 and meropenem-3 combinations were effective in murine peritonitis and neutropenic lung infection models caused by MDR Acinetobacter baumannii. Compounds 1-3 are novel β-lactamase inhibitors that demonstate potent cross-class inhibition, and clin. studies targeting MDR infections are warranted. In the part of experimental materials, we found many familiar compounds, such as (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4Product Details of 194726-40-4)
(R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Product Details of 194726-40-4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem