Relebactam, also known as MK-7655, a potent and selective β-lactamase inhibitor. At a concentration of 4 mg/L, MK-7655 reduced imipenem MICs for Enterobacteriaceae with KPC carbapenemases from 16-64 mg/L to 0.12-1 mg/L. MK-7655 potentiated imipenem against Enterobacteriaceae with KPC carbapenemases or combinations of β-lactamase and impermeability, but not those with metallo-carbapenemases. It augmented the activity of imipenem against P. aeruginosa in general and OprD mutants in particular.
Mangion, Ian K.; Ruck, Rebecca T.; Rivera, Nelo; Huffman, Mark A.; Shevlin, Michael. A concise synthesis of a β-lactamase inhibitor. Organic Letters. Volume 13. Issue 20. Pages 5480-5483. Journal; Online Computer File. (2011).
Liu, Zhijian; Yasuda, Nobuyoshi; Simeone, Michael; Reamer, Robert A. N-Boc Deprotection and Isolation Method for Water-Soluble Zwitterionic Compounds. Journal of Organic Chemistry. Volume 79. Issue 23. Pages 11792-11796. Journal; Online Computer File. (2014).
Wankhede, Karuna Suresh; Surwase, Mahesh Manikrao; Bhawsar, Satish; Deshpande, Prasad Keshav; Yeole, Ravindra Dattatraya; Patel, Mahesh Vithalbhai. A process for preparation of (2S,5R)- sulfuric acid mono-{[(4-aminopiperidin-4-yl) carbonyl]-7-oxo-1,6-diazabicyclo[3.2.1]-oct-6-yl}ester. Assignee Wockhardt Limited, India. IN 296654. (2018
Gordon, Eric M.; Freund, John; Gallop, Mark A.; Duncton, Matthew Alexander James. Beta-lactamase inhibitors and uses thereof. Assignee Arixa Pharmaceuticals, Inc., USA. US 10085999. (2018).
Miller, Steven P.; Limanto, John; Zhong, Yong-Li; Yasuda, Nobuyoshi; Liu, Zhijian. Preparation of tert-butyl 4-((1R,2S,5R)-6- (benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carboxylate. Assignee Merck Sharp & Dohme Corp., USA. WO 2014200786. (2014).