This paper describes the discovery of alpha -trifluoroketoacetamides as pot
ent antibacterial agents against Gram-positive organisms. The initial SAR i
ndicates that the aryl ethyl side chain is essential in maintaining antibac
terial activity. The SAR observations have been utilized to design a bioiso
stere for the alpha -trifluoroketoacetamide with good activity against Gram
-positive organisms. (C) 2001 Elsevier Science Ltd. All rights reserved.