Synthesis and antibacterial evaluation of fused pyrazoles and Schiff bases |
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| Authors: | Ashraf S Hassan Gaber O Moustafa Ahmed A Askar Ahmed M Naglah Mohamed A Al-Omar |
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| Institution: | 1. Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt;2. Ashraf_salmoon@yahoo.com;4. Peptide Chemistry Department, National Research Centre, Cairo, Egypt;5. Botany and Microbiology Department Faculty of Science (Boys), Al-Azhar University, Cairo, Egypt;6. Drug Exploration and Development Chair (DEDC) Department of Pharmaceutical Chemistry College of Pharmacy, King Saud University, Riyadh, Saudi Arabia |
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| Abstract: | AbstractFor the discovery of new antibiotic drugs to face the problem of microbial resistance, a series of fused pyrazoles such as pyrazolopyrimidines 15a–f, pyrazoloquinazolines 18a, b and pyrazolotriazines 20a, b was synthesized via the reaction of 5-aminopyrazoles 8a, b with 3-(dimethylamino)-1-aryl-prop-2-en-1-ones 9a–d, 2-((dimethylamino)methylene)-5,5-dimethylcyclohexane-1,3-dione (16) and sodium nitrite (NaNO2), respectively. Finally, Schiff bases 22a–g were obtained by the condensation of 8a, b with aromatic aldehydes 21a–d. The chemical structure of the new compounds was confirmed by spectroscopy. The structure of 15?b was confirmed by X-ray crystallography analysis. All compounds were screened for antibacterial properties toward multi-drug resistant bacteria (MDRB). |
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| Keywords: | Antibacterial agent fused pyrazole Schiff base X-ray crystallography 5-aminopyrazole |
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