91622-14-9Relevant articles and documents
A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli
Goldberg, Joel A.,Nguyen, Ha,Kumar, Vijay,Spencer, Elizabeth J.,Hoyer, Denton,Marshall, Emma K.,Cmolik, Anna,O'Shea, Margaret,Marshall, Steven H.,Hujer, Andrea M.,Hujer, Kristine M.,Rudin, Susan D.,Domitrovic, T. Nicholas,Bethel, Christopher R.,Papp-Wallace, Krisztina M.,Logan, Latania K.,Perez, Federico,Jacobs, Michael R.,Van Duin, David,Kreiswirth, Barry M.,Bonomo, Robert A.,Plummer, Mark S.,Van Den Akker, Focco
, p. 5990 - 6002 (2020)
Treatment of multidrug-resistant Gram-negative bacterial pathogens represents a critical clinical need. Here, we report a novel γ-lactam pyrazolidinone that targets penicillin-binding proteins (PBPs) and incorporates a siderophore moiety to facilitate uptake into the periplasm. The MIC values of γ-lactam YU253434, 1, are reported along with the finding that 1 is resistant to hydrolysis by all four classes of β-lactamases. The druglike characteristics and mouse PK data are described along with the X-ray crystal structure of 1 binding to its target PBP3.
An approach to the synthesis of 5,5-trans-fused lactam analogues of β-lactam antibiotics
Smith, Paul W.,Whittington, Andrew R.,Cobley, Kevin N.,Jaxa-Chamiec, Albert,Finch, Harry
, p. 21 - 25 (2007/10/03)
A racemic synthesis of two diastereoisomeric α-benzyloxycarbonylamino substituted trans-fused bicyclic lactams (4 and 5), was achieved from cyclopentene oxide. These lactams are useful intermediates to investigate the possibility of using a trans-lactam t
