Results 61 to 70 of about 2,355 (106)
Truncation of Samroiyotmycin: Tailored seco‐Acids as Novel Antimalaria Compounds
Six truncated samroiyotmycin‐derived antimalarials were synthesized by replacing the tosyloxazole unit with electron‐deficient aryl groups. The most active seco‐acid with EWG = 2 × CF3 outperformed the natural product SamA. Its enhanced activity supports a donor–acceptor interaction involving the electron‐poor aryl unit, consistent with inhibition of ...
Anton Czuczkowski +10 more
wiley +1 more source
Three-dimensional QSAR studies for N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones were conducted using TSAR 3.3. The in vitro activities (MICs) of the compounds against Staphylococcus aureus ATCC 25923 exhibited a strong correlation with the ...
Neha Gandhi +7 more
core +1 more source
Primary amines reacted with carbonate salts (Na2CO3, K2CO3, Cs2CO3, and Ag2CO3) and halomethyloxiranes in the presence of a base such as DBU or TEA to give oxazolidinones in high yields.
Yoshihiro Ida (2677675) +6 more
core +1 more source
Photochemistry of oxazolidinones antibacterial drugs [PDF]
The photochemistry of six N3-(3-fluoro-4-dialkylaminophenyl)-oxazolidinones known for their antimicrobial activity has been examined. All of these compounds are defluorinated in water (dec ≈ 0.25) and in methanol (dec ≈ 0.03), reasonably via the triplet.
Angelo Albini +5 more
core +1 more source
Previously synthesized 1,3‐oxazolidine pyrimidine nucleoside analogues (S1–S6) were evaluated for HIV‐1 reverse transcriptase inhibition using molecular docking, ADMET prediction, and an in vitro colorimetric HIV‐RT assay. Compounds S4 and S5 exhibited the strongest binding affinities and moderate enzyme inhibition (IC50 = 19.27 and 22.80 µM ...
Shimoga Nagaraj Sriharsha +11 more
wiley +1 more source
Silica sulfuric acid catalyzes efficiently the reaction of carbamates and oxazolidinones with anhydrides under solvent-free conditions. All the reactions were done at room temperature and the N-acyl carbamates and oxazolidinones were obtained with high ...
Liqiang Wu, Xiaojuan Yang, Fulin Yan
doaj
(S)-4-Isopropyl-5,5-diphenyloxazolidin-2-one
(S)-4-Isopropyl-5,5-diphenyloxazolidin-2-one has been synthesized for the first time by the enantiospecific oxidative carbonylation of commercially available (S)-2-amino-3-methyl-1,1-diphenylbutan-1-ol.
Raffaella Mancuso +5 more
doaj +1 more source
Methamphetamine Enantiomers: From Chemical Synthesis to Biological Fate
Methamphetamine is an amphetamine‐type stimulant characterized by a single stereogenic center, resulting in two enantiomers, (R)‐(−)‐methamphetamine and (S)‐(+)‐methamphetamine, with distinct biological and pharmacological profiles. These forms exhibit differences in central nervous system activity, metabolism, excretion, and overall physiological ...
Larissa Pires do Espírito Santo +9 more
wiley +1 more source
A stereodivergent route from D‐mannitol enables access to enantiopure C5‐α‐substituted linezolid analogues with full configurational control. Biological evaluation reveals that α‐substitution abolishes antibacterial activity irrespective of stereochemistry, establishing a strict steric limitation at C5 and highlighting the dominant role of substituent ...
José A. Gálvez +3 more
wiley +1 more source
A novel series of benzisothiazole‐based hydrazide derivatives was designed, synthesized, and evaluated for antitubercular activity. Compound 8k emerged as the most potent candidate (MIC = 0.25 μg/mL) with a high selectivity index (SI = 42) and bactericidal activity. Molecular docking and 100 ns simulations identified InhA as the probable target.
Vivek Sharma +3 more
wiley +1 more source

