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Synthesis, Antimicrobial Activity, α-Amylase Inhibitory Tests and Molecular Docking Studies of Thiazole Based Hydrazones Derived from 2-acyl-(1H)-indene-1,3(2H)-diones

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Pharmaceutical Chemistry Journal Aims and scope

A series of new thiazole based hydrazones have been synthesized and their antimicrobial and α-amylase (type-II diabetes) inhibitory activities have been evaluated. The structures of synthesized derivatives were elucidated by various spectral techniques including FTIR, NMR and mass spectrometry. Antibacterial activity tests were performed against two Gram-positive (Bacillus subtilis and Staphylococcus aureus) and two Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacterial strains. Two fungal strains (Candida albicans and Aspergillus niger) were taken for testing antifungal activity. Among the tested derivatives, compound 3d was found to be the most potent against all tetsed bacterial and fungal strains. The α-amylase inhibitory activity of all compounds was also assayed using the starch iodine method. Derivatives 3j and 3k exhibited the best inhibitory activity against α-amylase enzyme with IC50 values of 0.26 ± 0.06 and 0.32 ± 0.02 μM, respectively, in comparison to acarbose (IC50 = 0.11 ± 0.00 μM) as standard reference. The results of the biological activity evaluation were confirmed by docking studies.

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CONFLICT OF INTEREST

The authors declare that they have no conflicts of interest.

Funding

The authors are grateful to the University Grants Commission (New Delhi, India) [Sr. No. 2061610093 Ref. No.19/06/2016(i)EU-V, dated 26-12-2016] and the Council of Scientific and Industrial Research (New Delhi, India) [CSIR no. 09/752(0060)/2016-EMR-I] and [CSIR no. 09/752(0104)/2019-EMR-I] for providing financial support.

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Authors and Affiliations

  1. Department of Chemistry, Guru Jambheshwar University of Science and Technology, 125001, Hisar, Haryana, India

    S. Mor, M. Khatri, S. Sindhu & R. Punia

  2. Department of Chemistry, Government College, 125001, Hisar, Haryana, India

    S. Nagoria

  3. Department of Bio and Nanotechnology, Guru Jambheshwar University of Science and Technology, 125001, Hisar, Haryana, India

    A. Kumar

  4. Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, 125001, Hisar, Haryana, India

    A. Kumar

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Correspondence to S. Mor.

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Mor, S., Khatri, M., Sindhu, S. et al. Synthesis, Antimicrobial Activity, α-Amylase Inhibitory Tests and Molecular Docking Studies of Thiazole Based Hydrazones Derived from 2-acyl-(1H)-indene-1,3(2H)-diones. Pharm Chem J 56, 925–934 (2022). https://doi.org/10.1007/s11094-022-02728-6

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