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Novel 3‐Substituted Ocotillol‐Type Triterpenoid Derivatives as Antibacterial Candidates
Author(s) -
Bi Yi,
Ma Cong,
Zhang Hengyuan,
Zhou Zhiwen,
Yang Jian,
Zhang Zhenlei,
Meng Qingguo,
Lewis Peter J.,
Xu Jinyi
Publication year - 2014
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12337
Subject(s) - bacillus subtilis , chloramphenicol , kanamycin , antibacterial activity , staphylococcus aureus , chemistry , antimicrobial , antibiotics , bacteria , triterpenoid , microbiology and biotechnology , traditional medicine , stereochemistry , biochemistry , biology , organic chemistry , medicine , genetics
Plant‐derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol‐type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μ g/mL against Staphylococcus aureus and 8 μ g/mL and 4 μ g/mL against Bacillus subtilis , respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub‐MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.