N-alkylated glycine trimers are generically referred to as peptoids. The id
entification of antimicrobial peptoids from a statistically unbiased divers
e combinatorial chemistry library led to the design of the optimization pep
toid library that we describe in this manuscript. This optimization library
was designed using structural information from the most active peptoids in
the unbiased library. Screening of the optimization library for antimicrob
ial activity identified a single pool of peptoids with activity against bot
h Staphylococcus aureus and Escherichia coli. The active peptoids from this
pool were active against drug sensitive and drug resistant organisms and r
epresent novel antibacterial compounds. (C) 1999 Elsevier Science Ltd. All
rights reserved.