Kirk, Ralph published the artcileNovel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections, Related Products of esters-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(20), 127428, database is CAplus and MEDLINE.
Delafloxacin, a fourth-generation anionic fluoroquinolone (FQ) was approved in 2019 for community acquired bacterial pneumonia (CARP). It has broad spectrum activity and an improved class-related toxicity profile. However, it has recently failed a Phase 3 clin. trial for treatment of N. gonorrhoeae infections due to the lack of sufficient efficacy at the dose administered. Inspired by the microbiol. and safety profile of delafloxacin, we have developed and profiled the first reported delafloxacin carbon analog whereby a Nitrogen-for-Carbon swap has been successfully carried out at the C7 position. Not only have we shown that compounds with this modification maintain activity against N. gonorrhoeae (plus other gram-pos. and gram-neg. bacteria) but they also demonstrate a differentiated physicochem. profile. A zwitterionic derivative of delafloxacin was also profiled and demonstrated a superior microbiol. profile against gram-neg. strains, while maintaining favorable selected ADMET properties.
Bioorganic & Medicinal Chemistry Letters published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Related Products of esters-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics