Synthesis, antimicrobial activities and GAPDH docking of new 1,2,3-triazole derivatives

Alkhaldi, A. A.M., Abdelgawad, M. A., Youssif, B. G.M., El-Gendy, A. O. and De Koning, H. (2019) Synthesis, antimicrobial activities and GAPDH docking of new 1,2,3-triazole derivatives. Tropical Journal of Pharmaceutical Research, 18(5), 1108. (doi:10.4314/tjpr.v18i5.27)

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Purpose: To synthesize new triazole derivatives in order to overcome the problem of side effects of antimicrobial agents and microbial resistance, while broadening the spectrum of antimicrobial activity. Methods: The starting triazole, compound 1, was prepared through click chemistry and reacted with chloroacetyl chloride to yield compound II. Triazole 1 was reacted with acids and aldehydes to produce oxadiazole (III) and azomethine (IV) which cyclized in acetic anhydride to give a new acetylated oxadiazole (V). Minimum inhibitory concentration (MIC) and resorufin assays were used for antibacterial and anti-parasitic screening, respectively. Compounds II and IVb were subjected to molecular docking studies using glyceraldehyde-3-phosphate dehydrogenase (GAPDH) Molecular Operating Environment (MOE) program. Results: Novel oxazole-triazole derivative (III) showed high activity against Pseudomonas aeruginosa and moderate activity against Staphylococcus epidermidis, whereas compound IVc showed moderate activity against Staphylococcus epidermidis. Chloro-acetyl-triazole II and 2-hydroxyphenyl-triazole Schiff base (Ivb) showed pronounced activity against the kinetoplastid parasites, Leishmania major, Leishmania mexicana and Trypanosoma brucei. Conclusion: The new synthesized triazoles represent a new antimicrobial scaffold and identifies potential new lead compounds for follow-up and for further mechanistic studies.

Item Type:Articles
Additional Information:The authors would like to thank Jouf University, KSA, for funding this research through research Grand Project no. 378/37.
Glasgow Author(s) Enlighten ID:De Koning, Professor Harry
Authors: Alkhaldi, A. A.M., Abdelgawad, M. A., Youssif, B. G.M., El-Gendy, A. O., and De Koning, H.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:Tropical Journal of Pharmaceutical Research
Publisher:Pharmacotherapy Group, University of Benin, Benin City
ISSN (Online):1596-9827
Copyright Holders:Copyright © 2019 The Authors
First Published:First published in Tropical Journal of Pharmaceutical Research 18(5):1108
Publisher Policy:Reproduced under a Creative Commons License

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