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Vol. 38 No. 6 (2026): Vol. 38 Issue No 6, 2026

Copyright (c) 2026 Solomon Attah, Chris OKORO, Vivian Okonkwo, Fidelia Ibeano, Cosmas Chinweike

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Synthesis of Medicinally Relevant Pro-Pro Dipeptide as Antidiabetic, Anti-inflammatory and Antioxidant: Molecular Docking and Drug-Likeness

https://doi.org/10.14233/ajchem.2026.35715
Solomon Izuchi Attah
Department of Pure and Industrial Chemistry, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0000-0002-4717-0774
Uchechukwu Chris Okoro
Department of Pure and Industrial Chemistry, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0000-0002-4116-7144
Ifeoma Vivian Okonkwo
Department of Science Laboratory Technology, Faculty of Physical Sciences, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0000-0003-3107-913X
Fidelia Ngozi Ibeanu
Department of Natural Science Unit, School of General Studies, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0000-0003-3194-1025
Precious Kelechi Attah
Department of Pure and Industrial Chemistry, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0009-0002-1429-6036
Cosmas Chinweike Eze
Department of Natural Science Unit, School of General Studies, University of Nigeria, Nsuuka, Nigeria
https://orcid.org/0000-0003-1205-4607

Corresponding Author(s) : Solomon Izuchi Attah

solomon.attah@unn.edu.ng

Asian Journal of Chemistry, Vol. 38 No. 6 (2026): Vol. 38 Issue No 6, 2026

Abstract

The choice of design and synthesis of new dipeptide derivatives is due to their broad pharmacological activities against various diseases. In present study, eight novel dipeptides incorporating sulphonamide functionality (8a-h) were synthesised via the reaction of benzenesulphonyl chloride and L-proline to afford benzenesulphonamides. The condensation reaction of benzenesulphonamides and carboxamide derivatives, using peptide coupling reagents afforded the dipeptide compounds (8a-h). The structural validation of the compounds was done using IR, 1H NMR, 13C NMR and MS spectrometry. Molecular docking studies revealed favourable interactions between the compounds and key amino acid residues in the active site of the protein targets. The drug-likeness study showed that the compounds comply with Lipinski’s rule of five, indicating strong potential as orally bioavailable candidates. Compound 8a exhibited superior antidiabetic activity compared to the standard clinical drug, acarbose. Antioxidant screening demonstrated that compound 8g, with an IC50 value of 0.214 µg/mL, exhibited comparable activity to ascorbic acid (IC50: 0.213 µg/mL). In the carrageenan-induced rat paw edema bioassay, at 0.5 h, compounds 8a-h showed strong anti-inflammatory inhibition with percentage inhibition in the range of 97.67-86.64 %, compared to the reference drug, indomethacin (75.55 %). Some of the dipeptide derivatives are identified as promising therapeutic agents for further studies.

Keywords

Dipeptides Benzenesulphonamides L-proline Biological activities Pharmacokinetics Toxicity properties
(1)
Attah, S. I.; Okoro, U. C.; Okonkwo, I. V.; Ibeanu, F. N.; Attah, P. K.; Eze, C. C. Synthesis of Medicinally Relevant Pro-Pro Dipeptide As Antidiabetic, Anti-Inflammatory and Antioxidant: Molecular Docking and Drug-Likeness. ajc 2026, 38, 1471-1481.
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