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Future Pharmacology
Volume 4
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10.3390/futurepharmacol4020023
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Article

Repurposing Synthetic Acetaminophen Derivatives Containing a Benzothiazole Scaffold as an Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species

by
Boniface Pone Kamdem
1,*,
Brice Rostan Pinlap
1,
Bijou-Lafortune Noumboue Kouamou
1,
Aubin Youbi Kamche
1,
Boris Arnaud Kuate
2,
Joseph Tsemeugne
2,*,
Orleans Ngomo
2,
Pierre Mkounga
2 and
Fabrice Fekam Boyom
1
1
Antimicrobial and Biocontrol Agents Unit (AmBcAU), Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon
2
Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon
*
Authors to whom correspondence should be addressed.
Future Pharmacol. 2024, 4(2), 420-436; https://doi.org/10.3390/futurepharmacol4020023
Submission received: 7 May 2024 / Revised: 15 June 2024 / Accepted: 17 June 2024 / Published: 20 June 2024
(This article belongs to the Special Issue Feature Papers in Future Pharmacology 2024)
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Abstract

Diarrhea remains one of the leading causes of mortality worldwide, especially among children. Accumulated evidence has shown that Shigella species are the most prevalent bacteria responsible for diarrhea in developing countries. Antimicrobial therapy is necessary for Shigella infections; however, the development of resistance against current drugs justifies the pressing need to search for alternative medications. In this study, we have applied antibacterial phenotypic screening to identify potent anti-Shigella compounds across a broad chemical diversity, including selected acetaminophen derivatives containing a benzothiazole backbone, and their combination with certain antibiotics. As a result, two acetaminophen derivatives containing a benzothiazole backbone (4a and 4b) inhibited the growth of Shigella flexneri with a common MIC value of 12.5 µg/mL. These compounds were established through a time-kill kinetics study to be potentially bactericidal. Meanwhile, the 2-aminobenzothiazoles (1a and 1b) used for the synthesis of compounds 4 (a and b) were found to be poorly active (MIC: 100 µg/mL) against this pathogen. Combination studies of 4a and 4b with the least effective antibiotics (ceftriaxone and cotrimoxazole) demonstrated synergistic anti-Shigella activity with MIC values decreasing from 12.5 to 0.781 μg/ mL. The present study demonstrates that the azobenzothiazole dyes 4 (a and b) can be repurposed as potential anti-Shigella compounds, thus providing potential chemical pharmacophores for the discovery of drugs against infectious diarrhea caused by Shigella and other enteric pathogens, especially in developing countries.
Keywords: acetaminophen; benzothiazoles; azo dyes; Shigella flexneri; anti-Shigella activity; repositioning; combination studies; diarrhea acetaminophen; benzothiazoles; azo dyes; Shigella flexneri; anti-Shigella activity; repositioning; combination studies; diarrhea

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MDPI and ACS Style

Pone Kamdem, B.; Pinlap, B.R.; Noumboue Kouamou, B.-L.; Youbi Kamche, A.; Kuate, B.A.; Tsemeugne, J.; Ngomo, O.; Mkounga, P.; Fekam Boyom, F. Repurposing Synthetic Acetaminophen Derivatives Containing a Benzothiazole Scaffold as an Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species. Future Pharmacol. 2024, 4, 420-436. https://doi.org/10.3390/futurepharmacol4020023

AMA Style

Pone Kamdem B, Pinlap BR, Noumboue Kouamou B-L, Youbi Kamche A, Kuate BA, Tsemeugne J, Ngomo O, Mkounga P, Fekam Boyom F. Repurposing Synthetic Acetaminophen Derivatives Containing a Benzothiazole Scaffold as an Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species. Future Pharmacology. 2024; 4(2):420-436. https://doi.org/10.3390/futurepharmacol4020023

Chicago/Turabian Style

Pone Kamdem, Boniface, Brice Rostan Pinlap, Bijou-Lafortune Noumboue Kouamou, Aubin Youbi Kamche, Boris Arnaud Kuate, Joseph Tsemeugne, Orleans Ngomo, Pierre Mkounga, and Fabrice Fekam Boyom. 2024. "Repurposing Synthetic Acetaminophen Derivatives Containing a Benzothiazole Scaffold as an Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species" Future Pharmacology 4, no. 2: 420-436. https://doi.org/10.3390/futurepharmacol4020023

APA Style

Pone Kamdem, B., Pinlap, B. R., Noumboue Kouamou, B.-L., Youbi Kamche, A., Kuate, B. A., Tsemeugne, J., Ngomo, O., Mkounga, P., & Fekam Boyom, F. (2024). Repurposing Synthetic Acetaminophen Derivatives Containing a Benzothiazole Scaffold as an Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species. Future Pharmacology, 4(2), 420-436. https://doi.org/10.3390/futurepharmacol4020023

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