1264296-84-5Relevant academic research and scientific papers
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
-
Paragraph 00247, (2020/12/11)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Metabolically stable tert-butyl replacement
Barnes-Seeman, David,Jain, Monish,Bell, Leslie,Ferreira, Suzie,Cohen, Scott,Chen, Xiao-Hui,Amin, Jakal,Snodgrass, Brad,Hatsis, Panos
, p. 514 - 516 (2013/07/26)
Susceptibility to metabolism is a common issue with the tert-butyl group on compounds of medicinal interest. We demonstrate an approach of removing all the fully sp3 C-Hs from a tert-butyl group: replacing some C-Hs with C-Fs and increasing the s-character of the remaining C-Hs. This approach gave a trifluoromethylcyclopropyl group, which increased metabolic stability. Trifluoromethylcyclopropyl-containing analogues had consistently higher metabolic stability in vitro and in vivo compared to their tert-butyl-containing counterparts.
