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Vol. 28 No. 8 (2016): Vol 28 Issue 8

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Certain 4-Iminoflavones Derivatives: Synthesis, Docking Studies, Antiasthmatic and Antimicrobial Agents

https://doi.org/10.14233/ajchem.2016.19789
Shaila Khah
School of Pharmaceutical Sciences, Shoolini University, Solan-173 212, India
Rohit Goyal
School of Pharmaceutical Sciences, Shoolini University, Solan-173 212, India
Ankush Chabba
School of Pharmaceutical Sciences, Shoolini University, Solan-173 212, India
Varun Jaiswal
School of Computer Science and Bioinformatics, Shoolini University, Solan-173 212, India
Gaurav Sharma
School of Chemistry, Shoolini University, Solan-173 212, India
Mu. Naushad
Department of Chemistry, College of Science, Building 5, King Saud University, Riyadh, Saudi Arabia

Corresponding Author(s) : Gaurav Sharma

gaurav8777@gmail.com

Asian Journal of Chemistry, Vol. 28 No. 8 (2016): Vol 28 Issue 8

Abstract

In this present study, certain substituted 4-iminoflavone derivatives 5(a-j) were synthesized. All the synthesized compounds were evaluated for antiasthmatic and antimicrobial activity. Among the synthesized compounds, 5f was found to be the most promising against asthmatic models, whilst, 5h was found active against all the microbial strains. Antiasthmatic activity was correlated and evaluated with various models, e.g., citric acid induced cough model, OVA induced asthma model (biochemical estimation for cell infiltrations, estimation of lipid peroxidation and glutathione and estimation of TNF-a and IL-6 and histamine induced response). Compound 5f was found to show 2.20 ± 0.047 number of cough whilst codeine showed 1.40 ± 0.548; compound 5f produced considerable reduction in neutrophils, lymphocytes, eosinophils and leukocytes; decrease in LPO level (lung and BALF) and increment in GSH level (lungand BALF); and decreased the level of TNF-a and IL-6, respectively. On the other hand, 5h showed MIC 6.25 μg/mL against B. subtilis and S. aureus, 3.1 μg/mL against E. coli, 1.55 μg/mL against S. typhi and 6.25 μg/mL against C. albicans, respectively. In addition to gain better understanding on the biological activities of synthesized compounds, molecular docking study was performed within the binding site of human histamine H1 receptor and Glc-6-P synthase revealing compound 5f and 5h as best fit within the respective receptor pockets.

Keywords

4-Iminoflavone Antiasthmatic Antimicrobial activity
Khah, S., Goyal, R., Chabba, A., Jaiswal, V., Sharma, G., & Naushad, M. (2016). Certain 4-Iminoflavones Derivatives: Synthesis, Docking Studies, Antiasthmatic and Antimicrobial Agents. Asian Journal of Chemistry, 28(8), 1687–1696. https://doi.org/10.14233/ajchem.2016.19789
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