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Title: Design, synthesis and antibacterial evaluation of 3-substituted ocotillol-type derivatives
Authors: Wang, KY
Zhou, ZW
Zhang, HY
Cao, YC
Xu, JY
Ma, C 
Meng, QG
Bi, Y
Issue Date: 2018
Source: Molecules, Dec. 2018, v. 23, no. 12, 3320, p. 1-15
Abstract: Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7-26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7-14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 g/mL against MRSA USA300 and 4 g/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.
Keywords: Triterpenoid saponin
Antibacterial activity
Structure-activity relationship
Publisher: Molecular Diversity Preservation International (MDPI)
Journal: Molecules 
ISSN: 1420-3049
DOI: 10.3390/molecules23123320
Rights: © 2018 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 (
The following publication Wang, K. Y., Zhou, Z. W., Zhang, H. Y., Cao, Y. C., Xu, J. Y., Ma, C., . . . Bi, Y. (2018). Design, synthesis and antibacterial evaluation of 3-substituted ocotillol-type derivatives. Molecules, 23(12), 3320, 1-15 is available at
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