Design, synthesis, and unraveling the antibacterial and antibiofilm potential of 2-azidobenzothiazoles: insights from a comprehensive in vitro study

Qadir, Tanzeela; Kanth, Saadat A.; Aasif, Mohammad; Fadul, Abdalla N.; Yatoo, Gulam N.; Jangid, Kailash; Mir, Mushtaq A.; Shah, Wajahat A.; Sharma, Praveen K.

doi:10.3389/fchem.2023.1264747

Cited by 4 publications

(1 citation statement)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Many small molecules that contain heterocyclic elements are of pharmaceutical application/potential thanks to their broad biological activity [2]. Heterocyclic compounds are rapidly increasing in number due to extensive synthetic research and their synthetic utility [3] and play diverse roles in pharmacy and medicine, including anti-cancer, antimicrobial (including anti-biofilm), and antiinflammatory actions, and they are a major focus in the organic chemistry literature [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial and Cytotoxic Activities of Water-Soluble Isoxazole-Linked 1,3,4-Oxadiazole with Delocalized Charge: In Vitro and In Vivo Results

Dudek,

Bąchor,

Drozd-Szczygieł

et al. 2023

IJMS

View full text Add to dashboard Cite

The distinct structure of cationic organic compounds plays a pivotal role in enhancing their water solubility, which in turn influences their bioavailability. A representative of these compounds, which contains a delocalized charge, is 5-amino-2-(5-amino-3-methyl-1,2-oxazol-4-yl)-3-methyl-2,3-dihydro-1,3,4-oxadiazol-2-ylium bromide (ED). The high-water solubility of ED obviates the need for potentially harmful solvents during in vitro testing. The antibacterial and antifungal activities of the ED compound were assessed in vitro using the microtiter plate method and a biocellulose-based biofilm model. Additionally, its cytotoxic effects on wound bed fibroblasts and keratinocytes were examined. The antistaphylococcal activity of ED was also evaluated using an in vivo larvae model of Galleria mellonella. Results indicated that ED was more effective against Gram-positive bacteria than Gram-negative ones, exhibiting bactericidal properties. Furthermore, ED demonstrated greater efficacy against biofilms formed by Gram-positive bacteria. At bactericidal concentrations, ED was non-cytotoxic to fibroblasts and keratinocytes. In in vivo tests, ED was non-toxic to the larvae. When co-injected with a high load of S. aureus, it reduced the average larval mortality by approximately 40%. These findings suggest that ED holds promise for further evaluation as a potential treatment for biofilm-based wound infections, especially those caused by Gram-positive pathogens like S. aureus.

show abstract