article · Antibiotics
Novel benzothiazole derivatives were evaluated for their antimicrobial properties against a range of bacterial and fungal pathogens to address the challenge of antibiotic resistance. Laboratory testing against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans, and Aspergillus niger demonstrated minimum inhibitory concentration values ranging from 25 to 200 micrograms per millilitre. Specific compounds, designated 3 and 4, exhibited high antibacterial and moderate antifungal performance, whereas compounds 10 and 12 showed moderate broad activity across all tested species. Further investigations revealed that certain derivatives suppressed the enzymatic activity of Escherichia coli dihydroorotase and blocked the dimorphic transition in Candida albicans. Active variants also caused the leakage of DNA and protein from Aspergillus niger spores. Molecular docking suggested that interactions within the dihydroorotase active site physically hinder substrate access, indicating that enzyme inhibition plays a role in these antimicrobial effects.
Rising levels of antibiotic resistance threaten global healthcare by reducing the efficacy of existing treatments. Identifying novel chemical structures that target essential bacterial and fungal processes provides potential avenues to counter resistant infections. Understanding how these benzothiazole derivatives inhibit bacterial enzymes and disrupt fungal cells helps guide the development of new treatments against challenging microbial pathogens.
This early-stage research could inform the development of new antimicrobial drugs aimed at pharmaceutical developers tackling resistant bacterial and fungal infections. The findings are based entirely on in vitro laboratory assays and computational molecular docking, placing any therapeutic product at an early discovery phase. Considerable pre-clinical testing, including safety and in vivo efficacy evaluations, would be required before these compounds could advance toward clinical application.
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The burden of antibiotic resistance necessitates a continued search for new antimicrobials. We evaluated the antimicrobial activities of novel benzothiazoles synthesized by our group. Antibacterial activity was evaluated in vitro in <i>Staphylococcus aureus</i>, <i>Bacillus subtilis</i>, and <i>Escherichia coli</i>, while the antifungal activity was tested in <i>Candida albicans</i> and <i>Aspergillus niger</i>, and expressed as the minimum inhibitory concentration (MIC; µg/mL). MIC values of benzothiazole compounds ranged from 25 to 200 µg/mL. Compounds 3 and 4 gave high antibacterial and moderate antifungal activities, while 10 and 12 showed moderate activity against all tested organisms. In addition, some benzothiazole compounds significantly suppressed the activity of <i>Escherichia coli</i> dihydroorotase and inhibited the dimorphic transition of <i>Candida albicans</i>. Moreover, the active benzothiazole compounds induced DNA and protein leakage in <i>Aspergillus niger</i> spores. Molecular interactions of benzothiazole derivatives with dihydroorotase revealed the formation of hydrogen bonds with the active site residues LEU222 or ASN44. Strong hydrophobic interactions of the bulky thiazole and naphthalene rings at the entrance to the active site might interfere with the access of substrates to their binding sites, which results in dihydroorotase inhibition. Thus, inhibition of dihydroorotase might contribute to the observed antimicrobial actions of these compounds.
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DOI: 10.3390/antibiotics9050221
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