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Title: Synthesis and antibacterial evaluation of novel 3-substituted ocotillol-type derivatives as leads
Authors: Bi, Y
Liu, XX
Zhang, HY
Yang, X
Liu, ZY
Lu, J
Lewis, PJ
Wang, CZ
Xu, JY
Meng, QG
Ma, C 
Yuan, CS
Issue Date: 2017
Source: Molecules, Apr. 2017, v. 22, no. 4, 590, p. 1-10
Abstract: 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 mu g/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.
Keywords: Ocotillol
Derivatives
Synthesis
Antibacterial activity
Synergistic effect
Publisher: Molecular Diversity Preservation International (MDPI)
Journal: Molecules 
ISSN: 1420-3049
DOI: 10.3390/molecules22040590
Rights: © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
The following publication 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, 4, 590,1-10 is available at https://dx.doi.org/10.3390/molecules22040590
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