Array synthesis of novel lipodepsipeptide.
Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity.
Siedlecki
James
J
Cubist Pharmaceuticals Inc., 65 Hayden Ave., Lexington, MA 02421, USA.
Hill
Jason
J
Parr
Ian
I
Yu
Xiang
X
Morytko
Michael
M
Zhang
Yanzhi
Y
Silverman
Jared
J
Controneo
Nicole
N
Laganas
Valerie
V
Li
Tongchuan
T
Li
Jianshi
J
Keith
Dennis
D
Shimer
George
G
Finn
John
J
D000478:Alkylation; D000577:Amides / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D017576:Daptomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D013293:Enterococcus faecalis / Q000187:drug effects; D016984:Enterococcus faecium / Q000187:drug effects; D008055:Lipids / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010084:Oxidation-Reduction; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry
D000577:Amides; D000900:Anti-Bacterial Agents; D008055:Lipids; D010456:Peptides, Cyclic; D010879:Piperazines; D013449:Sulfonamides; D000077489:Piperazine; D017576:Daptomycin