Recent insights into antibacterial potential of benzothiazole derivatives

Abstract

Antimicrobial resistance (AMR) is a worldwide concern among infectious diseases due to increased mortality, morbidity and treatment cost. According to WHO 2019 report, among the 32 antibiotics in the clinical trials, only six were classified as innovative and containing novel moiety. The remaining antibiotics from this list contain previously known moiety (WHO AMR 2019). Therefore, the development of novel antibiotics to control resistance problems is crucial. Benzothiazole derivatives are of great interest due to their wide range of biological activities and medicinal applications. Reported data indicated that benzothiazole derivatives displayed antibacterial activity by inhibiting the dihydroorotase, DNA gyrase, uridine diphosphate-n-acetyl enol pyruvyl glucosamine reductase (MurB), peptide deformylase, aldose reductase, casdihydrofolate reductase, enoyl acyl carrier protein reductase, dialkylglycine decarboxylase, dehydrosqualene synthase, dihydropteroate synthase and tyrosine kinase. The present review analyzed the synthesis, structure-activity relationship (SAR) and mechanism of action studies of benzothiazole derivatives as antibacterial agents reported by various research groups in the last five years (2018–2022). Different patents on the antimicrobial activity of benzothiazole derivatives have also been summarized. The finding of the present review will be beneficial for the researchers in the development of novel antibacterial molecules based on benzothiazole moiety. Graphical Abstract

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

“…However, selected structural modifications of acetaminophen with the benzothiazole ring have afforded pharmacologically active compounds with decreased nephrotoxicity as compared to the parent molecule, i.e., acetaminophen [29]. On the other hand, the antibacterial potential of benzothiazoles is undeniable, as an important number of recent reports have described their efficacy against pathogenic microbes via numerous mechanisms of action, such as the inhibition of reactive chemical species [30], inhibition of uridine diphosphate-n-acetyl enol pyruvyl glucosamine reductase [31], DNA gyrase inhibition [32,33], peptide deformylase inhibition [34], aldose reductase inhibition [35], dihydroorotase inhibition [36], casdihydrofolate reductase inhibition [37], enoyl acyl carrier protein reductase inhibition [38], dialkylglycine decarboxylase inhibition [39], dehydrosqualene synthase inhibition [40], DNA gyrase and tyrosine kinase inhibition [41] and dihydropteroate synthase inhibition [42] among others [43].…”

Synthesis, antimicrobial activity and molecular simulation of thiourea derivatives containing 6-carboalkoxybenzo[d]thiazole and d-glucose moieties

“…5 It is already known that benzothiazole derivatives have very interesting biologically activities. 6 On the other hand, it has long been known that benzothiazole and its derivatives have been used as precursors in the synthesis of many other bioactive compounds that carry benzothiazole ring. 7,8 Derivatives containing benzothiazole exhibit multiple inhibitory activities, 9,10 such as antimycobacterial, 11 antifungal, 12 antibacterial, 13 anticancer, 14 antiproliferative, 15 anti-oxidant, and anti-inflammatory activity.…”