Facile Heterocyclic Synthesis and Antibacterial Activity of Substituted Isoxazol‐5(4H)‐ones

Abstract

An efficient, simple, and green procedure for the synthesis of isoxazol‐5(4H)‐one derivatives are described here through a convenient one‐pot, three‐component reaction at room temperature. The title compounds are isolated in high to excellent yields and after short reaction times, and are characterized by various spectroscopic methods such as IR, 1H NMR, and 13C NMR. The synthesized compounds 4a–c and 4e–i were tested for their in vitro activity against a panel of Gram‐positive and Gram‐negative bacteria, demonstrating their ability to inhibit microorganisms with a zone of inhibition ranging from 15 to 30 mm, minimum inhibitory concentration between 250 and 900 μg/mL, and minimum bacterial concentration between 700 and 1000 μg/mL.

Potential Nitrogen-Based Heterocyclic Compounds for Treating Infectious Diseases: A Literature Review

“…The synthesized compounds were evaluated for their in vitro antibacterial activity against Enterococcus faecium (DSM 20477), E. coli (CECT 515) and Clostridium perfringens (CECT 486) using ampicillin and gentamicin as standard drugs. Among the synthesized compounds, the ones with 4-F, 2-OH and 4-CH 3 exhibited remarkable activity across all three bacterial strains [ 7 ]. The compounds also displayed better activity in comparison with the reference drugs, while remaining compounds indicated good activity, except for the one containing 4-N(CH 3 ) 2 , which exhibited complete retardation against all the bacterial strains.…”

“… Synthesis of 2-(9-chloro-2,3-dimethyl- 6,7-dihydro-5 H -benzo[ 7 ] annulen-8-yl)-3-(3-oxo-3-[piperazin-1-yl]propyl)thiazolidin-4-one derivatives. …”

“…These compounds encompass a higher number of drugs, most biomass, nucleic acids, synthetic dyes, and numerous natural products such as alkaloids, herbicides, vitamins, antibiotics, hormones, and pharmaceutics [ 6 ]. Heterocyclic compounds have tremendous importance for both organic and medical chemists, and the synthesis of such molecules always remains a challenge from both industrial and academic aspects [ 7 ]. Heterocyclic systems with different structures display various biologic activities because of diversities in their molecular structures [ 8 ].…”

Preparation of Nanocatalysts Using Deposition Precipitation with Urea: Mechanism, Advantages and Results

“…However, metal losses of around 15 % were found, which may be linked to the incomplete incorporation of Au into the support. Note also that the presence of Cl in the catalysts can be linked to their strong adsorption by the support and the complete elimination of nitrogen. Effect of the support zero charge point of the surface (PZC): The PZC is a crucial parameter in this preparation method 1, 2, 5, 67, 68. Using different support natures, such as TiO 2 , SiO 2 , Al 2 O 3 , and CeO 2 , causes an important deposition rate with comparable reduced sizes at whatever deposition time in all the supports except SiO 2 (see Tab.…”

“…Effect of the support zero charge point of the surface (PZC): The PZC is a crucial parameter in this preparation method 1, 2, 5, 67, 68. Using different support natures, such as TiO 2 , SiO 2 , Al 2 O 3 , and CeO 2 , causes an important deposition rate with comparable reduced sizes at whatever deposition time in all the supports except SiO 2 (see Tab.…”