In 2014,Starr, Jeremy; Brown, Matthew F.; Aschenbrenner, Lisa; Caspers, Nicole; Che, Ye; Gerstenberger, Brian S.; Huband, Michael; Knafels, John D.; Lemmon, M. Megan; Li, Chao; McCurdy, Sandra P.; McElroy, Eric; Rauckhorst, Mark R.; Tomaras, Andrew P.; Young, Jennifer A.; Zaniewski, Richard P.; Shanmugasundaram, Veerabahu; Han, Seungil published 《Siderophore receptor-mediated uptake of lactivicin analogs in Gram-negative bacteria》.Journal of Medicinal Chemistry published the findings.Reference of tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:
Multidrug-resistant Gram-neg. pathogens are an emerging threat to human health, and addressing this challenge will require development of new antibacterial agents. This can be achieved through an improved mol. understanding of drug-target interactions combined with enhanced delivery of these agents to the site of action. Here, the authors describe the first application of siderophore receptor-mediated drug uptake of lactivicin analogs as a strategy that enables the development of novel antibacterial agents against clin. relevant Gram-neg. bacteria. They report the first crystal structures of several sideromimic conjugated compounds bound to penicillin binding proteins PBP3 and PBP1a from Pseudomonas aeruginosa and characterize the reactivity of lactivicin and β-lactam core structures. Results from drug sensitivity studies with β-lactamase enzymes are presented, as well as a structure-based hypothesis to reduce susceptibility to this enzyme class. Finally, mechanistic studies demonstrating that sideromimic modification alters the drug uptake process are discussed. In the experiment, the researchers used many compounds, for example, tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Reference of tert-Butyl N,N’-diisopropylcarbamimidate)
tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Reference of tert-Butyl N,N’-diisopropylcarbamimidate
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