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Synthesis, analgesic, anti-inflammatory and in vitro antimicrobial activities of some novel isoxazole coupled quinazolin-4(3H)-one derivatives

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Abstract

A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H NMR, mass spectroscopy and bases of elemental analysis with the aim of developing potent analgesic, anti-inflammatory and antimicrobial agents. Tail-flick technique, carrageenan-induced foot paw edema test and agar streak dilution test were performed for screening analgesic, anti-inflammatory and in vitro antimicrobial activity respectively. Moreover all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Out of various synthesized compounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl) isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was found to be the most active compound.

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Acknowledgments

The authors gratefully acknowledge the Central Instrumentation Facility, IIT Chennai, India for the spectral analysis of the compounds used in this study. The authors are also wish to thank the management of Bapatla College of Pharmacy for providing infrastructure facilities to carry out this research work.

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Authors and Affiliations

  1. Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Bapatla, Andhra Pradesh, India

    Govindaraj Saravanan

  2. Medicinal Chemistry Research Laboratory, M.N.R. College of Pharmacy, Sangareddy, Andhra Pradesh, India

    Veerachamy Alagarsamy

  3. Research Laboratory, Hindu College of Pharmacy, Guntur, Andhra Pradesh, India

    Pandurangan Dineshkumar

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  1. Govindaraj Saravanan
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  2. Veerachamy Alagarsamy
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Correspondence to Govindaraj Saravanan.

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Saravanan, G., Alagarsamy, V. & Dineshkumar, P. Synthesis, analgesic, anti-inflammatory and in vitro antimicrobial activities of some novel isoxazole coupled quinazolin-4(3H)-one derivatives. Arch. Pharm. Res. 44, 1–11 (2021). https://doi.org/10.1007/s12272-013-0262-8

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