Assessment of Antimicrobial and Cytotoxic Activities of a Series of Uridine Derivatives
Sarkar M. A. Kawsar *
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Rubayea Yeasmin
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Sayed Tawhid Ahmed
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Mohammed Zawad Adnan Chowdhury
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Fatema Akter
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Meharun Nesa Khanom
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Khaled Hasan Jiam
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.
Yuki Fujii
Graduate School of Pharmaceutical Sciences, Nagasaki International University, 2825-7, Huis Tem Bosch, Sasebo, 859-3298 Nagasaki, Japan.
Yasuhiro Ozeki *
Graduate School of NanoBiosciences, Yokohama City University, 22-2, Seto, Kanazawa-ku, Yokohama, 236-0027, Japan.
*Author to whom correspondence should be addressed.
Abstract
Nucleoside analogues are promising candidates for the development of novel antimicrobial agents, with established applications in antiviral and anticancer therapies. Uridine (1), an essential component of RNA, serves as a key scaffold for biologically active derivatives. As part of an ongoing investigation into the synthesis of biologically significant nucleoside derivatives, this study presents a comprehensive evaluation of the antibacterial, antifungal, and toxicity activities of a series of uridine derivatives (2-13) bearing diverse biologically active acyl substituents within a unified molecular framework. The compounds (2–13) were evaluated for antibacterial activity against Gram-positive bacteria such as Bacillus subtilis and Bacillus cereus, and Gram-negative bacteria, including Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi, using the disc diffusion method. Antifungal activity was tested against Aspergillus niger and Rhizopus nigricans via the food poisoning technique, with inhibition measured by radial growth reduction. Toxicity was assessed through the brine shrimp lethality assay, and all results were compared with standard antibiotics, indicating the bioactivity potential of the synthesised compounds. From the antibacterial screening results, it was revealed that the test chemicals 4 and 6 significantly inhibited the growth of all Gram-positive and Gram-negative bacterial strains used. The inhibition of E. coli by 4 (14 mm), of S. typhi by 4 (15 mm), of B. subtilis by 6 (12 mm), and of B. cereus by 6 (14 mm) was remarkable. However, the test chemical 10 inhibited the highest mycelial growth of Rhizopus nigricans (60.0%) against all examined fungal pathogens. For comparative studies, two standard antibiotics, Ampicillin and Nystatin, were also determined. In addition to that, the toxicity results of brine shrimp lethality assay displayed the test chemicals 6, 7 and 8 with the highest levels of mortality (i.e., ~80% death) among all tested chemicals. Hence, uridine derivatives bearing various acyl substituents in the ribose moiety may represent good lead compounds for the future discovery of novel antibacterial and/or antifungal agents. It is anticipated that this study, employing uridine derivatives as test compounds, will contribute to further research toward the development of pesticides and therapeutic agents for the control of human and plant diseases.
Keywords: Uridine, antibacterial, antifungal, toxicity, inhibition