- Title
- Synthesis and antibacterial evaluation of novel 3-substituted ocotillol-type derivatives as leads
- Creator
- Bi, Yi; Liu, Xian-Xuan; Ma, Cong; Yuan, Chun-Su; Zhang, Heng-Yuan; Yang, Xiao; Liu, Ze-Yun; Lu, Jing; Lewis, Peter John; Wang, Chong-Zhi; Xu, Jin-Yi; Meng, Qing-Guo
- Relation
- Molecules Vol. 22, Issue 4
- Publisher Link
- http://dx.doi.org/10.3390/molecules22040590
- Publisher
- MDPI AG
- Resource Type
- journal article
- Date
- 2017
- Description
- 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.
- Subject
- ocotillol; derivatives; synthesis; antibacterial activity; synergistic effect
- Identifier
- http://hdl.handle.net/1959.13/1399817
- Identifier
- uon:34681
- Identifier
- ISSN:1420-3049
- 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/).
- Language
- eng
- Full Text
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