884199-50-2

Upstream product

• 884199-49-9 N-[1-(dimethylamino)ethylidene]-2,4-difluorobenzamide 
• 72482-64-5 2,4-difluorobenzoyl chloride 
• 118493-85-9 acetamide oxime 

Downstream Products

• 1448256-08-3 N-allyl-3-fluoro-4-(3’-methyl-1,2,4-oxadiazol-5'-yl)aniline 
• 1448255-94-4 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-(iodomethyl)oxazolidin-2-one 
• 1448255-96-6 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-(azidomethyl)oxazolidin-2-one 
• 1448256-12-9 3-(3’-fluoro-4’-(3”-methyl-1 ,2,4-oxadiazol-5-yl)-phenyl)-5-(aminomethyl)oxazolidin-2-one 
• 1448255-98-8 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-(N-acetylaminomethyl)oxazolidin-2-one 
• 1448256-00-5 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-(N-(thioacetyl)aminomethyl)oxazolidin-2-one 
• 1448256-02-7 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-((pyrazol-1-yl)methyl)oxazolidin-2-one 
• 1448256-04-9 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-((imidazol-1-yl)methyl)oxazolidin-2-one 
• 1448256-06-1 3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-((1,2,4-triazol-1-yl)methyl)oxazolidin-2-one 
• 1448256-10-7 tert-butyl N-allyl-(3-fluoro-4-(3’-methyl-1,2,4-oxadiazol-5’-yl)-phenyl)carbamate 

Relevant academic research and scientific papers

New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles

The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compounds, enantiomers separation and absolute configuration assignment. Experimental determination of the antibacterial activity of the designed (S)-1-((3-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea and (S)-1-((3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea against multidrug resistant linezolid bacterial strains was higher than that of linezolid.

NOVEL 1, 2, 4-OXADIAZOL COMPOUNDS ACTIVE AGAINST GRAM-POSITIVE PATHOGENS

The present invention relates to new oxazolidinone compounds of general formula (I) having antibiotic activity even against multiresistant bacterial strains (I).

New linezolid-like 1,2,4-oxadiazolesactive against Gram-positive multiresistant pathogens

The synthesis and the in vitro antibacterial activity of novel linezolid-like oxadiazoles are reported. Replacement of the linezolid morpholine C-ring with 1,2,4-oxadiazole results in an antibacterial activity against Staphylococcus aureus both methicillin-susceptible and methicillin-resistant comparable or even superior to that of linezolid. While acetamidomethyl or thioacetoamidomethyl moieties in the C(5) sidechain are required, fluorination of the phenyl B ring exhibits a slight effect on an antibacterial activity but its presence seems to reduce the compounds cytotoxicity. Molecular modeling performed using two different approaches - FLAP and Amber software - shows that in the binding pose of the newly synthesized compounds as compared with the crystallographic pose of linezolid, the 1,2,4-oxadiazole moiety seems to perfectly mimic the function of the morpholinic ring, since the H-bond interaction with U2585 is retained.

PYRROLIDINE DERIVATIVES AS HISTAMINE RECEPTORS LIGANDS

The present invention relates to pyrrolidine derivatives of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.