Synthesis, Molecular Docking and Biological Evaluation of Novel Chlorobenzenesulfonamide Analogues of Ibuprofen as Anti-Bacterial, Anti-Diabetic and Anti-Alzheimer Agents

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nThis is an unedited manuscript accepted for publication and provided as an Article in Press for early access at the author’s request. The article will undergo copyediting, typesetting, and galley proof review before final publication. Please be aware that errors may be identified during production that could affect the content. All legal disclaimers of the journal apply.n

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Year : 2025 [if 2224 equals=””]04/09/2025 at 2:57 PM[/if 2224] | [if 1553 equals=””] Volume : 03 [else] Volume : 03[/if 1553] | [if 424 equals=”Regular Issue”]Issue : [/if 424][if 424 equals=”Special Issue”]Special Issue[/if 424] [if 424 equals=”Conference”][/if 424] 01 | Page : 35 49

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    Adina Tatheer, Shahzad Murtaza, Naghmana Kausar, Hammad Ismail, Safeer Ahmed,

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  1. Researcher, Professor, Lecturer, Assistant Professor, Professor, Department of Chemistry, University of Gujrat, Hafiz Hayat Campus, Institute of Chemistry, KFUEIT, Rahim Yar Khan, Department of Chemistry, University of Gujrat, Hafiz Hayat Campus, Department of Biochemistry and Biotechnology, University of Gujrat, Department of Chemistry, Quaid-e-Azam University, Gujrat, Gujrat, Gujrat, Gujrat, Islamabad, Pakistan, Pakistan, Pakistan, Pakistan, Pakistan

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Abstract

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nIn this work, we have synthesized novel chlorobenzensulfonamide tertiary amide based analogues of Ibuprofen (Ibu) and investigated them for their anti-bacterial, anti-diabetic and anti-Alzheimer activities. In the first step, Ibu was converted to amide derivatives by incorporating different aromatic amines. These were further converted into sulfonamide analogues (Sul-Ibu, 1-9) by treating it with p-chlorobenzensulfonyl chloride. Sul-Ibu (1-9) were screened against S. aureus, B. subtilis, S. mutans, E. coli, P. aeruginosa, S. epidermidis, A. odontolyticus, B. halodurans, and M. luteus. The analogues 4, 7-9 showed significant results as compared to Ibu due to the presence of sulfonamide moiety. The anti-diabetic efficacy was also determined by testing the inhibitory potency against diabetes causing enzymes (α-amylase and α-glucosidase) and found 4 (IC50 61.80±0.85 µg/mL) and 5(IC50 53.75±0.79 µg/mL) as most promising agents. Sul-Ibu analogues also exhibited impressive inhibition profiles as Anti-Alzheimer agents. Compound 7 appeared to be the most potent one providing the percentage inhibition 95.8±0.31 against AChE and 96.7±0.16 against BChE. Additionally, this analogue also provided Ki value 27 µmol. Molecular docking study with α-amylase, α-glucosidase, AChE and BChE were also in good accordance to that of experimental results. These results clearly indicate that Sul-Ibu analogues appeared promising antibacterial, antidiabetic and anti-Alzheimer agents and should be considered for clinical studies.

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Keywords: Synthesis, anti-cholinesterase, anti-bacterial, anti-diabetic, α-amylase, α-glucosidase

n[if 424 equals=”Regular Issue”][This article belongs to International Journal of AgroChemistry ]

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[/if 424][if 424 equals=”Special Issue”][This article belongs to Special Issue under section in International Journal of AgroChemistry (ija)][/if 424][if 424 equals=”Conference”]This article belongs to Conference [/if 424]

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nAdina Tatheer, Shahzad Murtaza, Naghmana Kausar, Hammad Ismail, Safeer Ahmed. [if 2584 equals=”][226 wpautop=0 striphtml=1][else]Synthesis, Molecular Docking and Biological Evaluation of Novel Chlorobenzenesulfonamide Analogues of Ibuprofen as Anti-Bacterial, Anti-Diabetic and Anti-Alzheimer Agents[/if 2584]. International Journal of AgroChemistry. 04/09/2025; 03(01):35-49.

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nAdina Tatheer, Shahzad Murtaza, Naghmana Kausar, Hammad Ismail, Safeer Ahmed. [if 2584 equals=”][226 striphtml=1][else]Synthesis, Molecular Docking and Biological Evaluation of Novel Chlorobenzenesulfonamide Analogues of Ibuprofen as Anti-Bacterial, Anti-Diabetic and Anti-Alzheimer Agents[/if 2584]. International Journal of AgroChemistry. 04/09/2025; 03(01):35-49. Available from: https://journals.stmjournals.com/ija/article=04/09/2025/view=0

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Volume 03
[if 424 equals=”Regular Issue”]Issue[/if 424][if 424 equals=”Special Issue”]Special Issue[/if 424] [if 424 equals=”Conference”][/if 424] 01
Received 21/04/2025
Accepted 04/05/2025
Published 04/09/2025
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Publication Time 136 Days

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