Synthesis of new triazole fused imidazo[2,1-b]thiazole hybrids with emphasis on Staphylococcus aureus virulence factors

[Display omitted] A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a–u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited significant anti-biofilm act...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2019-10, Vol.29 (19), p.126621-126621, Article 126621
Hauptverfasser: Shareef, Mohd Adil, Sirisha, Kanugala, Sayeed, Ibrahim Bin, Khan, Irfan, Ganapathi, Thipparapu, Akbar, Syed, Ganesh Kumar, C., Kamal, Ahmed, Nagendra Babu, Bathini
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Sprache:eng
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Zusammenfassung:[Display omitted] A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a–u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited significant anti-biofilm activity with single and mixed biofilm disruption demonstrated by Field Emission Scanning Electron Microscope (FE-SEM). Furthermore, molecular docking studies revealed that they interact with the virulence factor, Staphylococcus aureus dehydrosqualene synthase (CrtM) (PDB ID: 2ZCS). Overall, the findings suggest compound 9c as potential lead for further development of novel antibacterial and anti-biofilm agents.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.08.025