Abstract:
:A series of novel pyridone conjugated monobactams with various substituents at the (4) position were synthesized and evaluated for their antibacterial activities against a panel of multidrug-resistant (MDR) Gram-negative bacteria in vitro. Compounds 46d, 54 and 75e displayed good to moderate activities against P. aeruginosa, among which the activity of 75e against P. aeruginosa was comparable to that of BAL30072 under iron limitation condition. Compounds 35, 46d, 54, 56a, 56c and 56d exhibited good to excellent antibacterial activities against E. coli and K. pneumoniae, which were comparable or superior to that of BAL30072. In vitro liver microsomal stability was further evaluated and the results manifested that Compounds 35, 46d and 54 were metabolically stable in human liver microsomes.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Kou Q,Wang T,Zou F,Zhang S,Chen Q,Yang Ydoi
10.1016/j.ejmech.2018.03.058subject
Has Abstractpub_date
2018-05-10 00:00:00pages
98-109eissn
0223-5234issn
1768-3254pii
S0223-5234(18)30301-5journal_volume
151pub_type
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