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.
Rigel Inc., 1180 Veterans Blvd., South San Francisco, CA 94080, USA.
Gary C
GC
Look
Charles
C
Vacin
Tracy M
TM
Dias
Sun
S
Ho
Thuy H
TH
Tran
Laurance L
LL
Lee
Cedric
C
Wiesner
Flora
F
Fang
Andrea
A
Marra
Don
D
Westmacott
Alexander E
AE
Hromockyj
Martin M
MM
Murphy
John R
JR
Schullek
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