Synthesis and antimicrobial activity of novel quinoline derivatives 3 bearing pyrazoline and pyridine analogues 4

7 Abstract The present investigation is in the interest of 8 some synthesized novel derivatives containing (3-(2-chlor9 oquinolin-3-yl)-5-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)(pyr10 idin-4-yl)methanones (4a–o) moieties incorporated with 11 different biological active heterocycles such as quinoline, 12 pyrazoline and pyridine derivatives. For the determination 13 of the compounds reported in this paper was based on IR, 14 H NMR, C NMR and mass spectral data and same 15 compounds were screened for their antibacterial and anti16 fungal activity on four bacteria (Staphylococcus aureus, 17 Streptococcus pyogenes, Escherichia coli, Pseudomonas 18 aeruginosa) and three fungi (Candida albicans, Aspergillus 19 niger, Aspergillus clavatus) using ampicillin and griseo20 fulvin as the standard drugs. Cytotoxicity study was carried 21 out using MTT colorimetric assay (HeLa cell line). Among 22 the screened compounds, 4e, 4f and 4n showed most potent 23 antibacterial activity, while compounds 4d and 4g emerged 24 as the most active against fungal strains. The results 25 demonstrated that compound 4o was remarkably active 26 against all microbial strains. From the viewpoint of SAR 27 studies, it was observed that the presence of electron 28 withdrawing groups remarkably enhanced the antimicrobial 29 activity of synthesized compounds. Additionally, pre30 liminary MTT cytotoxicity studies on HeLa cells suggested 31 that effective antimicrobial activity of 4e–g, 4n and 4o was 32 accompanied by low cytotoxicity Q1 .

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