Preparation of Some New Pyrazolo[1,5-a]pyrimidines and Evaluation of Their Antioxidant,Antibacterial (MIC and ZOI) Activities,and Cytotoxic Effect on MCF-7 Cell Lines |
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Authors: | Mohammad Mehdi Vahedi Prof?Dr Sakineh Asghari Prof?Dr Mahmood Tajbakhsh Dr Mojtaba Mohseni |
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Institution: | 1. Department of Organic Chemistry, Faculty of Chemistry, University of Mazandaran, Babolsar, 47416-95447 Iran;2. Department of Microbiology, University of Mazandaran, Babolsar, 47416-95447 Iran |
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Abstract: | This study aims to synthesize some novel pyrazolo1,5-a]pyrimidine derivatives, and investigate their biological activities. These compounds exhibited good to high antioxidant activities 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capabilities]. Among them, Ethyl 5-(2-ethoxy-2-oxoethyl)-7-hydroxy-2-methylpyrazolo1,5-a]pyrimidine-3-carboxylate ( 3h ) showed the highest antioxidant activity Half-maximal Inhibitory Concentration (IC50)=15.34 μM] compared to ascorbic acid (IC50=13.53 μM) as a standard compound. Their antibacterial activities were investigated against two Gram-positive bacteria (Bacillus subtilis, and Staphylococcus aureus) and two Gram-negative bacteria (Pseudomonas aeruginosa, and Escherichia coli). The results showed that Ethyl 7-hydroxy-5-phenylpyrazolo1,5-a]pyrimidine-3-carboxylate ( 3i ) has the best antibacterial activity against Gram-positive B. subtilis Zone of Inhibition (ZOI)=23.0±1.4 mm, Minimum Inhibitory Concentration (MIC)=312 μM]. Also, the cytotoxicity of these compounds was assessed against breast cancer cell lines human breast adenocarcinoma (MCF-7)], which 7-Hydroxy-2-methyl-5-phenylpyrazolo1,5-a]pyrimidine-3-carbonitrile ( 3f ) displayed the most cytotoxicity (IC50=55.97 μg/mL), in contrast with Lapatinib (IC50=79.38 μg/mL) as a known drug. |
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Keywords: | 5-amino pyrazole antibacterial antioxidant cytotoxicity pyrazolo[1 5-a]pyrimidine |
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