An efficient one-pot synthesis of thiochromeno[3,4-d]pyrimidines derivatives: Inducing ROS dependent antibacterial and anti-biofilm activities |
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| Affiliation: | 1. Department of Chemistry, National Institute of Technology, Warangal 506 004, Telangana, India;2. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500 007, Telangana, India;1. Biofilm Biology Laboratory, Centre for Research on Infectious Diseases (CRID), School of Chemical and Biotechnology, SASTRA University, Tirumalaisamudram, Thanjavur 613 401, Tamil Nadu, India;2. School of Chemical & Biotechnology, SASTRA University, Tirumalaisamudram, Thanjavur 613 401, Tamil Nadu, India;3. CARISM, SASTRA University, Tirumalaisamudram, Thanjavur 613 401, Tamil Nadu, India;4. Department of Biotechnology, Science Campus, Alagappa University, Karaikudi 630 003, Tamil Nadu, India;1. Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy;2. IEMEST, Istituto Euromediterraneo di Scienza e Tecnologia, via Emerico Amari, 123, 90139, Palermo, Italy;1. Biochemistry and Applied Microbiology Laboratory, Badji Mokhtar Faculty of Sciences, Department of Biology, Annaba University, Box 12 Sidi Amar, 23000 Annaba, Algeria;2. Molecular Bacteriology Laboratory, Institut Pasteur du Maroc, 1 Place Louis Pasteur, 20360 Casablanca, Morocco;3. Microbiology Laboratory, Faculty of Medicine and Pharmacy, 1 Street Hospital, 20360 Casablanca, Morocco;4. Resuscitation Center and Burns Treatment, University Hospital Ibn Rochd, 23000 Annaba, Algeria;5. Microbiology Laboratory, University Hospital Dorban, 23000 Annaba, Algeria |
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| Abstract: | An efficient synthesis of thiochromeno[3,4-d]pyrimidine derivatives has been achieved successfully via a one-pot three-component reaction of thiochrome-4-one, aromatic aldehyde and thiourea in the presence of 1-butyl-3-methyl imidazolium hydrogen sulphate [Bmim]HSO4. This new protocol has the advantages of environmental friendliness, high yields, short reaction times, and convenient operation. Furthermore, among all the tested derivatives, compounds 4b and 4c exhibited promising antibacterial, minimum bactericidal concentration and anti-biofilm activities against Staphylococcus aureus MTCC 96, Staphylococcus aureus MLS16 MTCC 2940 and Bacillus subtilis MTCC 121. The compound 4c also showed promising intracellular ROS accumulation in Staphylococcus aureus MLS16 MTCC 2940 comparable to that of ciprofloxacin resulting in apoptotic cell death of the bacterium. |
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| Keywords: | Ionic liquid Antibacterial activity Anti-biofilm Reactive Oxygen Species (ROS) |
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