1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study
| Autor: | Tarunkumar Nanjibhai Akhaja, Jignesh P. Raval |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Antifungal Agents
Indoles Stereochemistry Klebsiella pneumoniae Antitubercular Agents Bacillus subtilis Chemistry Techniques Synthetic Microbial Sensitivity Tests medicine.disease_cause Drug Discovery medicine Candida albicans Escherichia coli Pharmacology biology Chemistry Organic Chemistry Aspergillus niger Fungi General Medicine Mycobacterium tuberculosis biology.organism_classification Staphylococcus aureus Drug Design Antibacterial activity Aspergillus clavatus |
| Zdroj: | European journal of medicinal chemistry. 46(11) |
| ISSN: | 1768-3254 |
| Popis: | 1,3-dihydro-2H-indol-2-ones derivatives are reported to exhibit a wide variety of biodynamic activities such as antituberculer, anti HIV, fungicidal, antibacterial, anticonvulsant. These valid observations led us to synthesize some new indole-2-one derivative. Thus, herein we report synthesis of various 5-substituted-3-[{5-(6-methyl-2-oxo/thioxo-4-phenyl-1,2,3,4 tetrahydro pyrimidin-5-yl)-1,3,4-thiadiazol-2-yl}imino]-1,3-dihydro-2H-indol-2-one derivatives 4a–l using one pot multicomponent–Biginelli reaction via CaCl2 catalyst. Structures and purity of these compounds were confirmed by elemental, IR, (1H & 13C) NMR and Mass spectral analysis. Newly synthesized compounds were also tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv, in vitro antibacterial activity against selected human pathogens viz. Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Staphylococcus aureus, Staphylococcus pyogenus, Bacillus subtilis and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus clavatus strains. |
| Databáze: | OpenAIRE |
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