Compound 3b Lab Report

889 Words 4 Pages
Abstract
6- bromo-2-(4-chlorophenyl)quinazolin-4(3H)-one derivatives 2-7 were synthesized.. The synthesized compounds were evaluated for their anti-microbial activity using the agar diffusion technique . The tested compounds were evaluated against, Gram +ve bacteria , Gram -ve bacteria, Yeast and Filamentous Fungus. Minimum inhibitory concentration (MIC) was made in vitro for compounds which showed antimicrobial activity. Compound 3b has broad spectrum activity against Gram +ve bacteria, Gram -ve bacteria, Yeast and Filamentous Fungus with MICs 150, 150, 75, 312, 625 and 625 µg/mL against (Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 3555, Escherichia coli ATCC 23282 Pseudomonas aeruginosa ATCC 10145, Candida albicans IMRU
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Introduction Resistant bacterial strains has become a serious problem [1]. This is due to false diagnosis and the excessive use of antibiotic [2,3]. This encourage us to search for new antimicrobial agents. Quinazolinones are heterocycles that are of great interest due to their biological activities such as anticancer [4-8], anti-psychotic [9], anti-inflammatory [10,12], antifungal [12-14] and antimicrobial activities[15-18].

Many 2,3 disubstituted quinazolinone derivatives have good antimicrobial and antifungal activities [19,20]. On the other hand substitution at 3rd position of bromo quinazolinone derivatives with phenyl ring show potential antimicrobial and antifungal activities [21,22]. Chacones, pyrazole, isoxazole and thiopyrimidine have antibacterial and antifungal activities [23-26].
Continuation of our research program which aim to synthesis of new biologically active quinazolin-4-one derivatives [4-8, 22], we synthesized new bromo quinazolinone derivatives substituted at 3rd position with chalcones,pyrazole, isoxazole or thio pyrimidine moiety bearing para chloro phenyl moiety at position 2.

2. Results and discussion
2.1.
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6-bromo quinazolinone derivatives bearing para chloro phenyl moiety at position 2 and substituted at 3rd position with 4-chalcone moiety bearing 4-choro phenyl 3b show remarkable antimicrobial, anti yeast and anti fungal activity . 4-chalcone moiety bearing 3,4,5-trimethoxyphenyl 3d show potent activity against Gram -ve bacteria. On the other hand 4-chalcone moiety having phenyl or furan-2-yl abolish antimicrobial activity but have potent anti yeast and anti fungal activity. While substitution with 4-nitrophenyl at the same position afford compound 3c with no antimicrobial or antifungal activity. Substituted at 3rd position with 5-phenyl- pyrazol or 1-acetyl-5-phenyl moiety give compound 4a, 5a respectively with promising anti yeast and anti fungal activity. While substitution at the same position with 1-acetyl-(4-chlorophenyl) moiety give 5b which have potent activity against Gram +ve bacteria. Compounds 6a,b and 7a,b with dihydro isoxazol or thioxo-tetrahydro pyrimidinyl moiety repectively at 3rd position of quinazolinone nucleus has neither antimicrobial nor anti fungal

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