Convenient synthesis of novel 4-substitutedamino-5-trifluoromethyl–2,7-disubstituted pyrido[2,3-d] pyrimidines and their antibacterial activity
| Autor: | Banda Narsaiah, S. Ravi Kanth, U. Surya Narayana Murthy, P. Shanthan Rao, K. Hara Kishore, G. Venkat Reddy |
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| Rok vydání: | 2006 |
| Předmět: |
Pharmacology
Spectrometry Mass Electrospray Ionization Magnetic Resonance Spectroscopy Trifluoromethyl Gram-negative bacteria Spectrophotometry Infrared biology Stereochemistry Gram-positive bacteria Organic Chemistry Microbial Sensitivity Tests General Medicine Gram-Positive Bacteria biology.organism_classification Dimroth rearrangement Chemical synthesis Anti-Bacterial Agents chemistry.chemical_compound Pyrimidines chemistry Gram-Negative Bacteria Drug Discovery Antibacterial activity Amination Antibacterial agent |
| Zdroj: | European Journal of Medicinal Chemistry. 41:1011-1016 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2006.03.028 |
| Popis: | Novel pyrido[2,3-d]pyrimidines 4 have been synthesised starting from 2-amino-4-trifluoromethyl-6-substituted nicotinonitriles 1 via imine formation, selective amination followed by Dimroth rearrangement. Compounds 4 were screened against Gram +ve and -ve bacteria in vitro. Compounds 4h and 4d showed significant activity against all species of Gram positive bacteria and moderate activity against Gram negative bacteria. N-2,4 difluorophenyl compounds 4l and 4m were the least active among all the compounds. All the compounds were inactive against Pseudomonas aeruginosa at the maximum concentration of 200 microg ml(-1). |
| Databáze: | OpenAIRE |
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