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3-Aryl/Heteryl-5-Phenylindeno[1,2-d]thiazolo[3,2-a]pyrimidin-6(5H)-ones: Synthesis, Characterization, and Antimicrobial Investigation

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Abstract

Discovery towards the potent antimicrobial agents is indispensable for the treatment of infections caused by resistant microbes. Thus, we prepared a novel series of 3-substituted 5-phenylindeno-thiazolopyrimidinone derivatives following conventional method. All the molecules were investigated for their in vitro antimicrobial potency against different bacteria and fungi, and the results were compared with streptomycin and clotrimazole standard drugs, respectively. Among the twelve analogs, 4-methoxyphenyl-5-phenylindeno[1,2-d]thiazolo[3,2-a]pyrimidin-6(5H)-one showed equipotent activity against a bacterium, Staphylococcus aureus (minimum inhibitory concentration 25 µg/mL and zone of inhibition 22 mm), and a fungus, Aspergillus niger (zone of inhibition 20 mm). The rest of the thiazolo[3,2-a]pyrimidin-6(5H)-one derivatives exhibited week to reasonable activities against the tested bacterial and fungal strains.

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ACKNOWLEDGMENTS

The authors are grateful to Dr. Busi Siddhardha, Department of microbiology, Pondicherry University, for antimicrobial screening. Dr. Rajitha thanks the Department of Chemistry, Gayatri Vidya Parishad College of Engineering (A), A.P., for providing research facilities.

Funding

Arya C.G. thanks the MHRD for providing financial support.

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Authors and Affiliations

  1. Department of Chemistry, Gayatri Vidya Parishad College of Engineering (A), 530048, Andhra Pradesh, India

    G. Rajitha & U. Sujana Kumari

  2. Department of Chemistry, National Institute of Technology Calicut, 673601, Kerala, India

    C. G. Arya & B. Janardhan

  3. Department of Chemistry, Palamuru University, 509001, Mahabubnagar, Telangana State, India

    S. V. Laxmi

  4. Department of Chemistry, National Institute of Technology Warangal, 506004, Warangal, Telangana State, India

    G. Ramesh

  5. Division of Environmental Monitoring and Exposure Assessment (Air) Laboratory, ICMR-NIREH, 462030, Bhopal, Madhya Pradesh, India

    G. Ramesh

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  1. G. Rajitha
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  2. C. G. Arya
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  3. B. Janardhan
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  4. S. V. Laxmi
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Correspondence to B. Janardhan.

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Corresponding author: phone: 0091-0891-2535788; e-mail: janardhan@nitc.ac.in.

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Rajitha, G., Arya, C.G., Janardhan, B. et al. 3-Aryl/Heteryl-5-Phenylindeno[1,2-d]thiazolo[3,2-a]pyrimidin-6(5H)-ones: Synthesis, Characterization, and Antimicrobial Investigation. Russ J Bioorg Chem 46, 612–619 (2020). https://doi.org/10.1134/S106816202004007X

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