Alkylidene Oxapenem β-Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges

Autor:	John Breen, Minli Zhang, Kishore Reddy, Matthew D. Miller, Jeroen C. Verheijen, Sushmita D. Lahiri, Pravin S. Shirude, Tiffany Palmer, Sharon Tentarelli, Kale Manoj Ganpat, Mark Zambrowski
Jazyk:	angličtina
Rok vydání:	2014
Předmět:	chemistry.chemical_classification Broad spectrum Enzyme β lactamase inhibitor Stereochemistry Chemistry Organic Chemistry Drug Discovery Bioinformatics Biochemistry
Popis:	We present a comprehensive study of C6-alkylidene containing oxapenems. We show that this class of β-lactamase inhibitors possesses an unprecedented spectrum with activity against class A, C, and D enzymes. Surprisingly, this class of compounds displayed significant photolytic instability in addition to the known hydrolytic instability. Quantum mechanical calculations were used to develop models to predict the stability of new analogues.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7850ce841723882bd3d91f0f310123b5 https://europepmc.org/articles/PMC4137382/ Zobrazit plný text záznamu