Modifications of the C6-substituent of penicillin sulfones with the goal of improving inhibitor recognition and efficacy
M Nottingham, CR Bethel, SRR Pagadala…
文献索引：Nottingham, Micheal; Bethel, Christopher R.; Pagadala, Sundar Ram Reddy; Harry, Emily; Pinto, Abishai; Lemons, Zachary A.; Drawz, Sarah M.; Akker, Focco Van Den; Carey, Paul R.; Bonomo, Robert A.; Buynak, John D. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 387 - 393
In order to evaluate the importance of a hydrogen-bond donating substituent in the design of β-lactamase inhibitors, a series of C6-substituted penicillin sulfones, lacking a C2′ substituent, and having an sp3 hybridized C6, was prepared and evaluated against a representative classes A and C β-lactamases. It was found that a C6 hydrogen-bond donor is necessary for good inhibitory activity, but that this feature alone is not sufficient in this ...
