One pot solvent free synthesis and in vitro antitubercular screening of 3-Aracylphthalides against Mycobacterium tuberculosis

One pot solvent free synthesis and in vitro antitubercular screening of 3-Aracylphthalides against Mycobacterium tuberculosis

One pot synthesis of 3-Aracylphthalide was accomplished in good yield by reacting 2-carboxy benzaldehyde with various aromatic methyl ketones in presence of methane sulphonic acid. Various phthalides thus obtained were characterized with spectral techniques. These phthalides were subjected to in vit...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-02, Vol.23 (3), p.711-714
Hauptverfasser: Limaye, Rohan A., Kumbhar, Virendra B., Natu, Arun D., Paradkar, Madhusudan V., Honmore, Varsha S., Chauhan, Rubia R., Gample, Suwarna P., Sarkar, Dhiman
Format: Artikel
Sprache:eng
Schlagworte:
3-Aracylphthalide
Antitubercular activity
Antitubercular Agents - chemical synthesis
Antitubercular Agents - pharmacology
Aromatics
Benzaldehyde
Benzofurans - chemical synthesis
Benzofurans - chemistry
Benzofurans - pharmacology
chemistry
Drug Discovery
drugs
Humans
Inhibitory Concentration 50
ketones
Methane
Methane sulphonic acid
Molecular Structure
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
One pot synthesis
phthalides
screening
Solvents
sulfonic acid
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Zusammenfassung:One pot synthesis of 3-Aracylphthalide was accomplished in good yield by reacting 2-carboxy benzaldehyde with various aromatic methyl ketones in presence of methane sulphonic acid. Various phthalides thus obtained were characterized with spectral techniques. These phthalides were subjected to in vitro antitubercular screening against Mycobacterium tuberculosis H37Ra (MTB) by using XRMA protocol. Among the phthalides screened, four exhibited half maximal inhibitory concentration (IC50) in the range of 0.81–1.24μg/ml thereby providing potential lead compounds for future drug discovery studies.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.11.097