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Open AccessArticle

Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, 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 Applied Biology and Chemical Technology, and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China
Authors to whom correspondence should be addressed.
Molecules 2018, 23(12), 3320;
Received: 30 November 2018 / Revised: 12 December 2018 / Accepted: 13 December 2018 / Published: 14 December 2018
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 726 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 714, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/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. View Full-Text
Keywords: triterpenoid saponin; ocotillol; antibacterial activity; synthesis; structure-activity relationship triterpenoid saponin; ocotillol; antibacterial activity; synthesis; structure-activity relationship
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MDPI and ACS Style

Wang, K.-Y.; Zhou, Z.-W.; Zhang, H.-Y.; Cao, Y.-C.; Xu, J.-Y.; Ma, C.; Meng, Q.-G.; Bi, Y. Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives. Molecules 2018, 23, 3320.

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