Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/80479
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dc.contributor.authorWang, KYen_US
dc.contributor.authorZhou, ZWen_US
dc.contributor.authorZhang, HYen_US
dc.contributor.authorCao, YCen_US
dc.contributor.authorXu, JYen_US
dc.contributor.authorMa, Cen_US
dc.contributor.authorMeng, QGen_US
dc.contributor.authorBi, Yen_US
dc.date.accessioned2019-03-26T09:17:27Z-
dc.date.available2019-03-26T09:17:27Z-
dc.date.issued2018-
dc.identifier.citationMolecules, Dec. 2018, v. 23, no. 12, 3320, p. 1-15en_US
dc.identifier.issn1420-3049-
dc.identifier.urihttp://hdl.handle.net/10397/80479-
dc.description.abstractAntibiotic 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.en_US
dc.description.sponsorshipDepartment of Applied Biology and Chemical Technologyen_US
dc.language.isoenen_US
dc.publisherMolecular Diversity Preservation International (MDPI)en_US
dc.relation.ispartofMoleculesen_US
dc.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 (http://creativecommons.org/licenses/by/4.0/).en_US
dc.rightsThe 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 https://dx.doi.org/10.3390/molecules23123320en_US
dc.subjectTriterpenoid saponinen_US
dc.subjectOcotillolen_US
dc.subjectAntibacterial activityen_US
dc.subjectSynthesisen_US
dc.subjectStructure-activity relationshipen_US
dc.titleDesign, synthesis and antibacterial evaluation of 3-substituted ocotillol-type derivativesen_US
dc.typeJournal/Magazine Articleen_US
dc.identifier.spage1-
dc.identifier.epage15-
dc.identifier.volume23-
dc.identifier.issue12-
dc.identifier.doi10.3390/molecules23123320-
dc.identifier.isiWOS:000454523000270-
dc.identifier.scopus2-s2.0-85058725276-
dc.identifier.pmid30558186-
dc.identifier.artn3320-
dc.description.validate201903 bcrc-
dc.description.oapublished_final-
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