abstract |
Substrates for β-lactamase of general formula (I) in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R' is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R' is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, -CHR2OCO(CH¿2?)nCH3, -CHR?2¿OCOC(CH¿3?)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R?2¿ is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO¿2? and CH2; and Z' and Z' are linkers for the fluorescent donor and quencher moieties. Methods of assaying β-lactamase activity and monitoring expression in systems using β-lactamase as a reporter gene also are disclosed. |