Abstract
Chalcone (3) has been synthesized as a new chalcone derivative bearing benzofuran moiety at 1 position. Such chalcone was used as a model dielectrophile applied to react with some nucleophiles such as 5-amino pyrazoles, 5-amino-1,2,4-triazole, 2-aminobenzimidazole, and 6-uraciles under Michael reaction conditions and resulted in a new series of fused pyrimidines such as pyrazolo[1,5-a]pyrimidines 7a-e, [1,2,4]-triazolo[1,5-a]pyrimidine 9, pyrimido[1,2-a]benzimidazole 11, and synthesis of pyrido[2,3-d]pyrimidinones 13a and b. The structures of the synthesized target heterocyclic compounds were confirmed by microanalytical and spectral data such as Fourier transform (FT)-IR, (1)H-NMR, and MS spectra. The newly synthesized compounds were evaluated for their anti-inflammatory and antimicrobial activities; most showed significant activities.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Aspergillus niger / drug effects
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Benzofurans / chemistry
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Benzofurans / pharmacology*
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Candida albicans / drug effects
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Carrageenan
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Dose-Response Relationship, Drug
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Edema / chemically induced
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Edema / drug therapy*
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Escherichia coli / drug effects
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Fusarium / drug effects
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Mice
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Microbial Sensitivity Tests
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Molecular Structure
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Pseudomonas aeruginosa / drug effects
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Staphylococcus aureus / drug effects
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Anti-Inflammatory Agents, Non-Steroidal
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Antifungal Agents
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Benzofurans
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Pyrimidines
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Carrageenan