https://nova.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 Synthesis and antibacterial evaluation of novel hydrophilic ocotillol-type triterpenoid derivatives from 20(S)-protopanaxadiol https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:28155 Staphylococcus aureus (CA-MRSA; strain USA300). From this series, compounds 6 and 15 were found to be the most active, both with MIC values of 2 µg/mL against B. subtilis 168 and 8 µg/mL against S. aureus USA300, respectively. Furthermore, subsequent assays showed that compounds 6 and 15 displayed strong synergistic effects at sub-MIC levels against both S. aureus USA300 and B. subtilis 168 when combined with two commercial antibiotics, kanamycin and chloramphenicol. Preliminary structure-activity relationship studies were also performed.]]> Wed 11 Apr 2018 12:07:46 AEST ]]> Synthesis and antibacterial evaluation of novel 3-substituted ocotillol-type derivatives as leads https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:34681 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.]]> Wed 04 Sep 2019 10:06:26 AEST ]]> Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:20628 Sat 24 Mar 2018 07:55:47 AEDT ]]> Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19340 in vitro antibacterial activity against several representative pathogenic bacterial strains. Compounds 20(S)-protopanaxadiol (PPD), 3, 5, 16 and 24 exhibited potent antibacterial activity against Gram-positive bacteria. Compounds 3 and 5 also displayed promising antibacterial activity against a community associated methicillin-resistant Staphylococcus aureus (CA-MRSA; strain USA300). Furthermore, compounds PPD, 3 and 16 combined with two commercially available antibiotics kanamycin and chloramphenicol showed strong synergistic inhibitory effects at their sub-MIC concentrations against S. aureus USA300 and Bacillus subtilis 168. Additionally, cytotoxic activity assay showed that the compounds tested did not affect cell viability of the human epithelial kidney (HEK-293) and human cervical (HeLa) cells at their MICs.]]> Sat 24 Mar 2018 07:52:12 AEDT ]]> Design, synthesis and in vitro NO-releasing activities of ocotillol-type furoxans https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:28246 1, II3, II4, III2 displayed higher potency in releasing NO at this concentration. Analysis of the in vitro data showed that the derivatives bearing the same furoxan group on different ocotillol cores possessed various NO releasing capacity, suggesting that the structure of carrier of NO releasing groups may affect the NO release. Indeed, except compound II2, 24(S)-6-deoxy ocotillol derivatives from compound 6 with different furoxan substitutions at 3-OH and III2 displayed enhanced NO releasing capacity, compared to other compounds derived from compounds 5 and 9. The results illustrated that the functional group and the stereochemistry on the ocotillol structure may affect the NO release of furoxans.]]> Sat 24 Mar 2018 07:28:32 AEDT ]]> Design, synthesis, nitric oxide release and antibacterial evaluation of novel nitrated ocotillol-type derivatives https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:28338 Sat 24 Mar 2018 07:25:14 AEDT ]]>