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Synthesis and antibiofilm evaluation of 3-hydroxy-2,3-dihydroquinazolin-4(1H)-one derivatives against opportunistic pathogen Acinetobacter baumannii
Institution:1. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China;2. Department of Biochemistry, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117596, Singapore;3. The Second People''s Hospital of Guizhou Province, Department of Pharmacy, Guiyang 550004, China;1. College of Chemistry & Chemical Engineering, Shaanxi University of Science & Technology, Xi’an, Shaanxi 710021, PR China;2. Key Laboratory of Auxiliary Chemistry & Technology for Chemical Industry, Ministry of Education, Xi’an, Shaanxi 710021, PR China;1. Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China;2. NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Science, Beijing 100050, China;3. Jiamusi University, Heilongjiang Province, China;1. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, PR China;2. College of Pharmacy, Guizhou Medical University, Guiyang, 550025, PR China;3. Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang, 550004, PR China;4. College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, PR China;1. Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, Telangana, India;2. Medicinal Chemistry and Biotechnology Division (MCB), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 007, India;3. Academy of Scientific and Innovative Research (AcSIR), New Delhi, India;4. Bioinformatics Division, PGRRCDE, Osmania University, Hyderabad 500007, India
Abstract:The emergence of multidrug resistant microorganisms has triggered the impending need for new aitimicrobial strategies. The antivirulence strategy with the benefite of alleviating the drug resistance becomes the focus of research. In this study, 22 quorum sensing inhibitors were synthesized by mimicking the structure of autoinducer and acinetobactin and up to 34% biofilm inhibition was observed with 5u. The biofilm inhibition effect was further demonstrated with extracellular polysaccharides inhibition and synergism with Gentamycin sulphate.
Keywords:Biofilm inhibition  Acinetobacter baumannii  Synthesis  Opportunistic pathogen  Drug resistance
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