Synthesis and in vitro antitubercular activity of some chroman derivatives

R. K. Kushwaha,Kuldeep Singh, D. Chandra,P. Kumar

Annals of phytomedicine(2022)

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摘要
Chromans are significant heterocyclic substances that can be created in a lab and are also naturally present in plants. They serve as a form of therapy such as antibreast cancer, antiestrogens, antitubercular and anticonvulsant, etc. The derivatives (ethyl 4-(substituted-2-hydroxyphenyl)-7-hydroxy-2-methyl-4H-chromene-3-carboxylate) were successfully synthesized using the intermediate ethylbenzylidine oxabutanoate. The proposed mechanism of the reaction is the Michael addition reaction. The resorcinol molecule functions as a nucleophile and the ethyl benzylidine oxabutanoate acts as a conjugated diene. These two compounds interact with one another to produce chroman derivatives. For the synthesis of benzopyran, this plan is highly efficient. Using autodock freeware software, designed compounds were studied for their antitubercular activity with target protein (InhA) enoyl-acyl carrier protein reductase (4fdo) receptor. According to a docking study, every compound has antitubercular activity. The drug isoniazid was used as standard in the biological studies for in vitro antitubercular activity on the MTB H37Rv strain. At the result of the assay, the pink color in the wells shows bacterial growth, whereas the blue color in the wells shows no bacterial growth. The minimum inhibitory concentration (MIC) was calculated. No MIC was seen in the in vitro antitubercular activity study up to the concentration of 64 mu g/ml.
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antitubercular activity,synthesis
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