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ID: ALA4396937

Journal: Bioorg Med Chem Lett

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

Authors: Shareef MA, Sirisha K, Sayeed IB, Khan I, Ganapathi T, Akbar S, Ganesh Kumar C, Kamal A, Nagendra Babu B.

Abstract: 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.

CiteXplore: 31431360

DOI: 10.1016/j.bmcl.2019.08.025