Copyright (c) 2025 Mo. Shahanawaz, Kuldeep Singh, Suvaiv, Syed Misbahul Hasan, Praveen Kumar, Arun Kumar, Iffat Zareen Ahmad
This work is licensed under a Creative Commons Attribution 4.0 International License.
Design and Synthesis of Novel Coumarin-Piperazine Derivatives as Potential Antimicrobial Agents
Corresponding Author(s) : Kuldeep Singh
Asian Journal of Chemistry,
Vol. 37 No. 4 (2025): Vol 37 Issue 4, 2025
Abstract
Coumarin piperazine acetamide analogues have shown great potential as drug candidates due to their wide range of biological activities. A series of novel coumarin-piperazine derivatives were synthesized and performed the in vitro antibacterial activity and ADME profiling. Compounds MS1, MS2, MS5 and MS6 exhibited docking scores higher than the standard ranging from -8.6 to -7.6 Kcal mol-1. Compound MS6 showed the best zone of inhibition, measuring 17 mm at 150 µg/mL against Staphylococcus epidermidis. Molecular docking and in vitro study of compound suggest that the presence of halogen on the aromatic ring, attached to piperazine might responsible for a good antibacterial potential. ADME profiling of the synthesized compounds showed the log S ESOL value between -2.39 to -4.52, number of H bond acceptors between 4-5, No. of H bond donors 1, high GIT absorption and adhered to the Lipinski, Ghose and Veber drug-likeness rules.
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S. Sandhu, Y. Bansal, O. Silakari and G. Bansal, Bioorg. Med. Chem., 22, 3806 (2014); https://doi.org/10.1016/j.bmc.2014.05.032
M. Garland, S. Loscher and M. Bogyo, Chem. Rev., 117, 4422 (2017); https://doi.org/10.1021/acs.chemrev.6b00676
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M.V. Kulkarni, G.M. Kulkarni, C.H. Lin and C.M. Sun, Curr. Med. Chem., 13, 2795 (2006); https://doi.org/10.2174/092986706778521968
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J. Chen, Y. Yu, S. Li and W. Ding, Molecules, 21, 1501 (2016); https://doi.org/10.3390/molecules21111501
L. Balewski, S. Szulta, A. Jaliñska and A. Kornicka, Front. Chem., 9, 781779 (2021); https://doi.org/10.3389/fchem.2021.781779
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M. Asif, Int. J. Adv. Sci. Res., 1, 05 (2015); https://doi.org/10.7439/ijasr.v1i1.1766
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D. Patel, R. Patel, P. Kumari and N. Patel, Med. Chem. Res., 21, 1611 (2012); https://doi.org/10.1007/s00044-011-9676-3
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