Abstract
A new series of 2, 3-disubstituted quinazolin4(3H)one derivatives was synthesized in good yield with the use of different aldehydes and evaluate their antimicrobial and anti-inflammatory activities. Disubstituted quinazolin4(3H)one derivatives were synthesized from Semicarbazide Hydrochloride and semicarbazone as starting materials through oxadiazole as intermediates. This intermediate on reaction with benoxazinone in acidic media, finally converted into corresponding 2, 3-disubstituted quinazolinone derivatives. The synthesized compounds were characterized by their physical properties, Infra-red (IR), nuclear magnetic resonance (NMR), Mass spectroscopic (MS) and elemental analysis and evaluated for biological activities. Ten different analogues of 2, 3-disubstituted quinazolin4(3H)one were successfully synthesized. All the compounds were active against microbial growth and inflammation. They all give good to moderate result on comparison with standard drug. The results reveal that pharmacological activity of quinazolin4(3H)one nucleus can be increased much times on chemical modification. This is advantageous to approaching the treatment of different kinds of severe diseases.
Highlights
It is well documentated that several bacteria and fungi pathogens have developed antibiotic resistance to various classes of antibiotics since past 30 years
Owing to the biological implication of these classes of compounds, we synthesized a series of 4(3H)-quinazoliones containing substituted styryl group at C-2 position & oxadiazoles at C-3 position and screened for antimicrobial by cup plate agar diffusion method and the zone of inhibition for each micro-organism at different concentrations and anti-inflammatory activities
All the synthesized compounds were characterized by modern analytical techniques
Summary
It is well documentated that several bacteria and fungi pathogens have developed antibiotic resistance to various classes of antibiotics since past 30 years. In view of the rapid increase in the multi-drug resistant (MDR) strains of pathogens, the need to search for new. Quinazolinone nucleus (Fig.1) present in many biologically active compounds is known to posses anticancer [3, 4] antibacterial [5], antitubercular [6], antifungal [7], anthelmintic [8], anti-HIV [9], anti-inflammatory [10], antitumor [11], antihypertensive activities [12], antiproliferative [13], antiulcer [14] and inhibitory effects for thymidylate synthase [15]. Owing to the biological implication of these classes of compounds, we synthesized a series of 4(3H)-quinazoliones containing substituted styryl group at C-2 position & oxadiazoles at C-3 position and screened for antimicrobial by cup plate agar diffusion method and the zone of inhibition for each micro-organism at different concentrations and anti-inflammatory activities
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