The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: modifications at C12 and C7
| Autor: | Hai-Xia Lin, Wen-Ming Zhang, Zhaobing Gao, Teng Yang, Yong-Mei Cui, Xue-Ying Pan, Xin-Lan Liu, Cai-Guang Yang |
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| Rok vydání: | 2017 |
| Předmět: |
Staphylococcus aureus
Stereochemistry Chemistry Techniques Synthetic 010402 general chemistry medicine.disease_cause 01 natural sciences Structure-Activity Relationship chemistry.chemical_compound Minimum inhibitory concentration Drug Discovery medicine Moiety Pharmacology Trifluoromethyl Strain (chemistry) 010405 organic chemistry Organic Chemistry General Medicine Oxime Drug Resistance Multiple humanities Anti-Bacterial Agents 0104 chemical sciences Multiple drug resistance chemistry Drug Design Abietanes Antibacterial activity human activities |
| Zdroj: | European Journal of Medicinal Chemistry. 127:917-927 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2016.11.002 |
| Popis: | A series of 7-N-acylaminoethyl/propyloxime derivatives of dehydroabietic acid were synthesized and investigated for their antibacterial activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Most of the target compounds having trifluoromethyl phenyl/benzyl, halogen-substituted thiophenyl, benzothiophenyl or pyrrolyl moiety exhibited potent in vitro antibacterial activity. Among which, compounds 4m, 4x and 7j showed high antibacterial activity with minimum inhibitory concentration (MIC) values of 1.25–3.13 μg/mL against five multidrug-resistant S. aureus. |
| Databáze: | OpenAIRE |
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