247115-23-7Relevant academic research and scientific papers
Catechol-based inhibitors of bacterial urease
Pagoni, Aikaterini,Daliani, Theohari,Macegoniuk, Katarzyna,Vassiliou, Stamatia,Berlicki, ?ukasz
supporting information, p. 1085 - 1089 (2019/03/07)
Targeted covalent inhibitors of urease were developed on the basis of the catechol structure. Forty amide and ester derivatives of 3,4-dihydroxyphenylacetic acid, caffeic acid, ferulic acid and gallic acid were obtained and screened against Sporosarcinia pasteurii urease. The most active compound, namely propargyl ester of 3,4-dihydroxyphenylacetic acid exhibited IC50 = 518 nM andkinact/Ki = 1379 M?1 s?1. Inhibitory activity of this compound was better and toxicity lower than those obtained for the starting compound – catechol. The molecular modelling studies revealed a mode of binding consistent with structure-activity relationships.
The synthesis and evaluation of 6-alkylidene-2'β-substituted penam sulfones as β-lactamase inhibitors
Buynak, John D.,A Srinivasa, Rao,Doppalapudi, Venkata Ramana,Adam, Greg,Petersen, Peter J.,Nidamarthy, Sirishkumar D.
, p. 1997 - 2002 (2007/10/03)
Penicillin sulfones, which structurally incorporate both a 6-position alkylidene substituent and a 2'β substituent, have been synthesized and evaluated as inhibitors of class C and class A serine β-lactamases. Incorporation of the 2'β-substituent generall
