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

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

  • Bioorg Med Chem Lett. 2019 Oct 1;29(19):126621. doi: 10.1016/j.bmcl.2019.08.025.
Mohd Adil Shareef 1,  Kanugala Sirisha 2,  Ibrahim Bin Sayeed 2,  Irfan Khan 2,  Thipparapu Ganapathi 3,  Syed Akbar 4,  C Ganesh Kumar 2,  Ahmed Kamal 5,  Bathini Nagendra Babu 6
Affiliations

Affiliations

  • 1 Centre for Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Tarnaka, 500007 Hyderabad, India; Academy of Scientific and Innovative Research, Ghaziabad 201002, India.
  • 2 Academy of Scientific and Innovative Research, Ghaziabad 201002, India; Organic Synthesis and Process Chemistry Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 3 Stem Cell Research Division, National Institute of Nutrition (NIN), Indian Council of Medical Research (ICMR), Hyderabad 500007, Telangana, India.
  • 4 Centre for Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Tarnaka, 500007 Hyderabad, India.
  • 5 School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110062, India. Electronic address: pvc@jamiahamdard.ac.in.
  • 6 Centre for Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Tarnaka, 500007 Hyderabad, India; Academy of Scientific and Innovative Research, Ghaziabad 201002, India. Electronic address: bathini@iict.res.in.
PMID: 31431360 DOI: 10.1016/j.bmcl.2019.08.025
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.

Keywords

Antimicrobial; Fused; Imidazo[2,1-b]thiazole; Staphylococcus aureus; Triazole; Virulence factors.

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