1174021-10-3Relevant articles and documents
Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin
Blizzard, Timothy A.,Chen, Helen,Kim, Seongkon,Wu, Jane,Bodner, Rena,Gude, Candido,Imbriglio, Jason,Young, Katherine,Park, Young-Whan,Ogawa, Aimie,Raghoobar, Susan,Hairston, Nichelle,Painter, Ronald E.,Wisniewski, Doug,Scapin, Giovanna,Fitzgerald, Paula,Sharma, Nandini,Lu, Jun,Ha, Sookhee,Hermes, Jeff,Hammond, Milton L.
, p. 780 - 785 (2014/02/14)
β-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C β-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C β-lactamases in vitro. It effectively restored imipenem's activity against imipenem-resistant Pseudomonas and Klebsiella strains at clinically achievable concentrations. A combination of MK-7655 and Primaxin is currently in phase II clinical trials for the treatment of Gram-negative bacterial infections.