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Molecules 2017, 22(4), 590;

Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China
State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
Department of Microbiology, The Chinese University of Hong Kong, Prince of Wales Hospital, Shatin, Hong Kong, China
Biological Sciences, School of Environmental and Life Sciences, University of Newcastle, Callaghan, NSW 2308, Australia
Tang Center for Herbal Medicine Research, the University of Chicago, Chicago, IL 60637, USA
Department of Anesthesia and Critical Care, The University of Chicago, Chicago, IL 60637, USA
Department of Applied Biology and Chemical Technology, and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Daniela Barlocco
Received: 1 March 2017 / Revised: 31 March 2017 / Accepted: 3 April 2017 / Published: 7 April 2017
(This article belongs to the Special Issue Frontiers in Antimicrobial Drug Discovery and Design)
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Due 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
Keywords: ocotillol; derivatives; synthesis; antibacterial activity; synergistic effect ocotillol; derivatives; synthesis; antibacterial activity; synergistic effect

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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.

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