Starting with a micromolar lead identified from high-throughput screening, a series of pyrazoles were discovered with significantly improved potency on bacterial methionyl-tRNA synthetase and selectivity over human methionyl-tRNA synthetase.

N-Acylated ornithine analogues of daptomycin were synthesized and tested for their antibacterial efficacy.

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.

L'invention concerne de nouveaux composes lipopeptidiques. Elle concerne egalement des compositions pharmaceutiques constituees par ces composes, ainsi que des procedes d'utilisation de ces composes en tant que composes antibacteriens. Elle concerne egalement des procedes servant a preparer ces nouveaux composes lipopeptidiques, et les intermediaires mis en application dans la preparation de ces composes.

La presente invention concerne de nouveaux composes lipopeptidiques. Elle concerne egalement des compositions pharmaceutiques obtenues de ces composes, et des methodes d'utilisation de ces composes comme agents antibacteriens. Elle concerne enfin des methodes de production des nouveaux composes lipopeptidiques, et des intermediaires utilises dans la production de ces composes.

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Steroidal derivatives as IL-1 beta release inhibitors are discussed.