Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads
AbstractDue to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2–16 µg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI < 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity. View Full-Text
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Bi, Y.; Liu, X.-X.; Zhang, H.-Y.; Yang, X.; Liu, Z.-Y.; Lu, J.; Lewis, P.J.; Wang, C.-Z.; Xu, J.-Y.; Meng, Q.-G.; Ma, C.; Yuan, C.-S. Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads. Molecules 2017, 22, 590.
Bi Y, Liu X-X, Zhang H-Y, Yang X, Liu Z-Y, Lu J, Lewis PJ, Wang C-Z, Xu J-Y, Meng Q-G, Ma C, Yuan C-S. Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads. Molecules. 2017; 22(4):590.Chicago/Turabian Style
Bi, Yi; Liu, Xian-Xuan; Zhang, Heng-Yuan; Yang, Xiao; Liu, Ze-Yun; Lu, Jing; Lewis, Peter J.; Wang, Chong-Zhi; Xu, Jin-Yi; Meng, Qing-Guo; Ma, Cong; Yuan, Chun-Su. 2017. "Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads." Molecules 22, no. 4: 590.
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