tetracycline and dehydroabietic-acid

Topics: Abietanes; Animals; Anti-Bacterial Agents; Drug Resistance, Multiple, Bacterial; Drug Stability; Microbial Sensitivity Tests; Oximes; Rats; Rats, Sprague-Dawley; Staphylococcus aureus; Structure-Activity Relationship

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.

Topics: Abietanes; Anti-Bacterial Agents; Chemistry Techniques, Synthetic; Drug Design; Drug Resistance, Multiple; Staphylococcus aureus; Structure-Activity Relationship

A series of 12-oxime and O-oxime ether derivatives of dehydroabietic acid were synthesized and investigated for the antibacterial activity against Staphylococcus aureus Newman strain and five multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The aromatic oximate derivative 11a showed the highest activity with MIC of 0.39-0.78μg/mL against S. aureus Newman. Of note, compounds 10b, 11 and 14 showed the most potent antibacterial activity against five multidrug-resistant S. aureus with MIC values of 1.25-3.13μg/mL. These results offered useful information for further strategic optimization in search of the antibacterial candidates against infection of multidrug-resistant Gram-positive bacteria.

Topics: Abietanes; Anti-Bacterial Agents; Drug Resistance, Multiple, Bacterial; Humans; Microbial Sensitivity Tests; Oximes; Staphylococcal Infections; Staphylococcus aureus; Structure-Activity Relationship