The discovery of biaryl acids and amides exhibiting antibacterial activity against Gram-positive bacteria.
Solid-phase synthetic methods for biaryl-based compounds were developed resulting in the construction of two 1000-member libraries. Numerous compounds were identified by high-throughput screening using whole cell screens to exhibit anti-microbial activity against Gram-positive bacteria. A series of biaryl compounds containing natural and unnatural amino acids were made to explore the SAR of the amino acid functionality.
Look
Gary C
GC
Rigel Inc., 1180 Veterans Blvd., South San Francisco, CA 94080, USA.
Vacin
Charles
C
Dias
Tracy M
TM
Ho
Sun
S
Tran
Thuy H
TH
Lee
Laurance L
LL
Wiesner
Cedric
C
Fang
Flora
F
Marra
Andrea
A
Westmacott
Don
D
Hromockyj
Alexander E
AE
Murphy
Martin M
MM
Schullek
John R
JR
D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects* / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000254:growth & development
D000577:Amides; D000596:Amino Acids; D000900:Anti-Bacterial Agents