Synthesis and biofilm inhibition studies of 2-(2-amino-6-arylpyrimidin-4-yl)quinazolin-4(3H)-ones |
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Affiliation: | 1. Department of Chemistry, Poornaprajna College, Udupi, Karnataka, India;2. Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Mysore, Karnataka, India;3. Department of Chemistry, MDRPU Science College, Mysore, Karnataka, India;4. PG Department of Chemistry, JSS College for Women, Mysuru, Karnataka, India |
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Abstract: | Synthesis of novel 4(3H)-quinazolinonyl aminopyrimidine derivatives has been achieved via quinazolinonyl enones which in turn were obtained from 2-acyl-4(3H)-quinazolinone. They have been assayed for biofilm inhibition against Gram-positive (methicillin-resistant Staphylococcus aureus (MRSA)) and Gram-negative bacteria (Acinetobacter baumannii). The analogues with 2,4,6-trimethoxy phenyl, 4-methylthio phenyl, and 3-bromo phenyl substituents (5h, 5j & 5k) have been shown to inhibit biofilm formation efficiently in MRSA with IC50 values of 20.7–22.4 μM). The analogues 5h and 5j have demonstrated low toxicity in human cells in vitro and can be investigated further as leads. |
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Keywords: | Aminopyrimidine Anti-biofilm MRSA biofilm |
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