Quinazolinone class of compounds is known to be an important chemical class with varied biological activities of pharmaceutical importance. They possess a variety of biological effects including antihypertensive, antimicrobial, anti-hyperlipidemic, antioxidant, anti-inflammatory, anticonvulsant, and anticancer activities1. Interest in quinazolinones has further increased since the report of compounds I and II as potent anti-bacterial agents. While compound I is found to be a potent Lpxc inhibitor2, compound II has been reported to be an inhibitor of penicillin binding protein PBP2a3. Inhibition of Lpxc leads to bactericidal activity against gram negative bacteria. Compound II and its related derivatives have been found to be inhibitors of methicillin-resistant S.aureus (MRSA). A new library of quinazolinone derivatives have been synthesized utilizing the structural features from the above two series of compounds and are evaluated against gram negative, gram positive bacteria and mycobacterium. The structure Activity Relationships will be discussed.

Design, synthesis and biological evaluation of new quinazolinone derivatives as potent antimicrobial agents

254th National Meeting (2017)

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