Broad spectrum antimicrobial, anti-inflammatory and peripheral analgesic activities of heteroaryl nitazoxanide analogs | ||||
| Egyptian Pharmaceutical Journal | ||||
| Volume 23, Issue 2, April 2024, Page 348-358 PDF (6.15 MB) | ||||
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| Authors | ||||
| S. M. Abdur Rahman; Tasmia Ahmed; Muhammad Asaduzzaman; Fahad Imtiaz Rahman; A. K. Azad Chowdhury | ||||
| Abstract | ||||
| Background The antiparasitic drug nitazoxanide possesses diverse biological activity. However, very few investigation was accomplished with nitazoxanide analogs. Therefore, herein we focused on the screening of bioactivities using some nitazoxanide-like synthesized molecules. Objectives Four heteroaryl nitazoxanide analogs synthesized in our laboratory were investigated for antimicrobial, anti-inflammatory, and analgesic activity. Materials and methods Disc diffusion method was used for assessing antimicrobial potency against several Gram-positive bacteria, Gram-negative bacteria, and fungi. Carrageenan-induced rat paw edema model was performed to evaluate anti-inflammatory activity. The analgesic property was evaluated using the acetic acid-induced writing inhibition method in the mice model. Molecular docking simulations against cyclooxygenase-1, cyclooxygenase-2, phospholipase A2, NF-κB inducing kinase, and interleukin-1 receptor-associated kinase 4 were also performed. Results and conclusion All the synthesized compounds exhibited broad spectrum antimicrobial property against a number of Gram-positive, Gram-negative species and unicellular fungi. Compound 4 or N-(5-nitrothiazol-2-yl)-furan-3-carboxamide emerged as the most prominent antimicrobial agent exhibiting zone of inhibition ranging in 14–22 mm. These zone diameters are sometimes greater than that displayed by nitazoxanide. Compounds 2 and 3 also showed remarkable broad-spectrum antimicrobial activity with a zone of inhibition 10–20 mm and 12–20 mm, respectively. Compound 4 also displayed potential anti-inflammatory activity which is comparable to standard aceclofenac. Compound 4 also showed mild analgesic effects. The compounds also exhibited moderate binding affinities against the selected target receptors and enzymes during in silico molecular docking. Heteroaryl nitazoxanide analogs showed prominent broad-spectrum antimicrobial, anti-inflammatory, and mild analgesic properties. This study indicates that heteroaryl nitazoxanide analogs might be interesting candidates for new drug discovery. | ||||
| Keywords | ||||
| Anti-inflammatory; Antimicrobial; broad-spectrum; Nitazoxanide; peripheral analgesic | ||||
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