The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: modifications at C12 and C7

• DOI: 10.1016/j.ejmech.2016.11.002
• Publication Date: 2016-11-03T08:46:25Z
• Authors: Wen-Ming Zhang; Teng Yang; Xue-Ying Pan; Xin-Lan Liu; Hai-Xia Lin; Zhao-Bing Gao; Cai-Guang Yang; Yong-Mei Cui
• Keywords: Moiety

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.