ABSTRACT
Constrained ceramide analogs were designed and synthesized by binding terminal alcohol and amine of ceramide with additional carbonyl functional group as 3-acetyl (3), 3-propionyl (4), 3-benzoyl (5), and 3-hexadecanoyl-4-(1-hydroxyhexadec-2-enyl)-oxazolidin-2-ones (6). Compounds 4 and 5 showed potent antileukemic activities against human leukemia HL-60 cells with good correlation between cell death and DNA fragmentation.
Subject(s)
Ceramides/chemical synthesis , Leukemia/pathology , Apoptosis/drug effects , Ceramides/pharmacology , Drug Screening Assays, Antitumor , Electrophoresis, Agar Gel , HL-60 Cells , HumansABSTRACT
A series of 4-arylpiperazin-1-yl-3-phenyloxazolidin-2-one derivatives with diversification of the N-substituents such as methylene O-linked heterocycles, thioamide, dithiocarbamate, thiourea, and thiocarbamate were synthesized and evaluated as antibacterial agents. Their in vitro activities (MIC) were evaluated against MRSA and VRE resistant Gram-positive strains such as Staphylococcus and Enterococcus. Most of the compounds were more potent in vitro but less active in vivo than linezolid.
Subject(s)
Oxazolidinones/chemical synthesis , Oxazolidinones/pharmacology , Piperazines/chemical synthesis , Piperazines/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Enterococcus faecalis/drug effects , Microbial Sensitivity Tests , Models, Molecular , Molecular Conformation , Oxazolidinones/chemistry , Piperazines/chemistry , Staphylococcus/drug effects , Structure-Activity RelationshipABSTRACT
A new naphthalene derivative containing a urea group at the 1,8-position of naphthalene was synthesized and showed a unique absorption and fluorescence peak with a fluoride ion. Calculations suggested that a new peak was attributed to the increased anion character of urea nitrogen due to the strong interaction of the fluoride and N-H protons.
