SYNTHESIS OF 4-(3H)-QUINAZOLINONES FOR POTENTIAL ANTIMICROBIAL ACTIVITY

Abstract

Quinazolinones are of considerable research interest since their discovery and are found in large numbers as naturally occurring alkaloids. They are reported to exhibit a wide range of useful biological activities like antibacterial, antiviral, antimalarial, anticancer, anticonvulsant, antihypertensive, antidiabetic, antihistamine and anti-inflammatory. There are several new reports on quinazolinone analogues showing a diverse spectrum of biological activities. A new series of 2-styryl 4(3H)- quinazolinone analogues were synthesized using anthranilamide, acetyl chloride and substituted aromatic benzaldehyde. The synthesized analogues (IVa-IVj) were purified by chromatography and characterized by spectroscopy. They were screened for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Pseudomonas vulgaris, Staphylococcus aureus and Bacillus subtilis using moxifloxacin as the reference standard and for antifungal activity against Candida albicans and Aspergillus niger using ketoconazole as the reference standard. The results indicated that IVa and IVj were active against E. coli, IVd against B. subtilis, IVb against S. aureus and IVa, IVb and IVe against C. albicans. The synthesized analogues did not exhibit activity against A. niger. The 2-styryl 4(3H)- quinazolinone series was found to show good activity against the selected bacterial strains and can serve as good templates for design and synthesis of more potent antibacterial and antifungal entities.