1998
DOI: 10.1039/a704097k
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Aminoalkylphosphinate inhibitors of D-Ala-D-Ala adding enzyme

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Cited by 86 publications
(43 citation statements)
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“…EF6265 was synthesized in our laboratory with consideration of the previously reported methods (Baylis et al, 1984;Miller et al, 1998;Vassiliou et al, 1999). Detailed procedures and spectroscopic data will be reported on another occasion.…”
Section: Methodsmentioning
confidence: 99%
“…EF6265 was synthesized in our laboratory with consideration of the previously reported methods (Baylis et al, 1984;Miller et al, 1998;Vassiliou et al, 1999). Detailed procedures and spectroscopic data will be reported on another occasion.…”
Section: Methodsmentioning
confidence: 99%
“…Phosphinate transition-state analogs of the MurC to -F enzymes were synthesized by various groups in the 1990s, and some of these showed potent enzyme inhibition (at low nanomolar levels for some, illustrating druggability of the targets) but no antibacterial activity, presumably due to a lack of cell entry (127,254,310,362,403). A number of inhibitors of MurB, -C, -D, and -F, found via screens for enzyme inhibition or binding, had micromolar (in some cases, low micromolar) 50% inhibitory concentrations (IC 50 s) and no (or weak in one case [370]) antibacterial activity (11,30,103,141,364,370).…”
Section: Murb To Murf Enzymes As Antibacterial Targetsmentioning
confidence: 99%
“…Previously described inhibitors of MurF include phosphinate transition state analogs (K i ϭ 200 to 700 M) (14) and the nonhydrolyzable ATP analog AMP-PCP [adenylyl 5Ј-(␤,␥-methylenediphosphonate)] (K ii ϭ 4 M) (1). Aside from per- Gu et al (10) and the thiazolylaminopyrimidine series described herein lacked measurable antibacterial activity.…”
Section: Discussionmentioning
confidence: 99%