Wu, Yachuang published the artcileOptimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria, Safety of tert-Butyl thiomorpholine-4-carboxylate, the main research area is biaryloxazolidinone preparation antibacterial; Antibiotic-resistant infections; Biaryloxazolidinone; Gram-positive bacteria; Structural optimization.
Herein, novel biaryloxazolidinone analogs I [X = O, S, NMe, etc.; Y = N, CH, CHOH, etc.; Z = N, CH] were designed and synthesized to improve the chem. and metabolic stability. Compounds I [X = S, NMe, SO2; Y = N, CHOH; Z = CH] showed significant antibacterial activity against the tested Gram-pos. bacteria as compared to radezolid and linezolid. Further studies indicated that most of them exhibited improved water solubility and chem. stability. Compound I [X = SO2; Y = N; Z = CH] had MIC values of 0.125-0.25 μg/mL against all tested Gram-pos. bacteria, and showed excellent antibacterial activity against clin. isolates of antibiotic-susceptible and antibiotic-resistant bacteria. Moreover, it was stable in human liver microsome. From a safety viewpoint, it showed non-cytotoxic activity against hepatic cell and exhibited lower inhibitory activity against human MAO-A compared to linezolid. The potent antibacterial activity and all these improved drug-likeness properties and safety profile suggested that compound I [X = SO2; Y = N; Z = CH] might be a promising drug candidate for further investigation.
European Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 220655-09-4 belongs to class thiomorpholine, name is tert-Butyl thiomorpholine-4-carboxylate, and the molecular formula is C9H17NO2S, Safety of tert-Butyl thiomorpholine-4-carboxylate.
Referemce:
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem