43043-31-8Relevant articles and documents
Structural optimization and antibacterial evaluation of rhodomyrtosone B analogues against MRSA strains
Zhao, Liyun,Liu, Hongxin,Huo, Luqiong,Wang, Miaomiao,Yang, Bao,Zhang, Weimin,Xu, Zhifang,Tan, Haibo,Qiu, Sheng-Xiang
supporting information, p. 1698 - 1707 (2018/10/26)
Methicillin-resistant Staphylococcus aureus (MRSA) infections are well-known as a significant global health challenge. In this study, twenty-two congeners of the natural antibiotic rhodomyrtosone B (RDSB) were synthesized with the aim of specifically enhancing the structural diversity through modifying the pendant acyl moiety. The structure-activity relationship study against various MRSA strains revealed that a suitable hydrophobic acyl tail in the phloroglucinol scaffold is a prerequisite for antibacterial activity. Notably, RDSB analogue 11k was identified as a promising lead compound with significant in vitro and in vivo antibacterial activities against a panel of hospital mortality-relevant MRSA strains. Moreover, compound 11k possessed other potent advantages, including breadth of the antibacterial spectrum, rapidity of bactericidal action, and excellent membrane selectivity. The mode of action study of compound 11k at the biophysical and morphology levels disclosed that 11k exerted its MRSA bactericidal action by membrane superpolarization resulting in cell lysis and membrane disruption. Collectively, the presented results indicate that the novel modified RDSB analogue 11k warrants further exploration as a promising candidate for the treatment of MRSA infections.
A test for homology: Photoactive crystalline assemblies involving linear templates based on a homologous series of phloroglucinols
Friscic, Tomislav,Drab, David M.,MacGillivray, Leonard R.
, p. 4647 - 4650 (2007/10/03)
(Chemical Equation Presented) Cocrystallization of trans-1,2-bis(4-pyridyl) ethylene (4,4′-bpe) with eight members of a homologous series of phloroglucinols 1a-h yields molecular solids 2(1a-h)·2(4,4′-bpe) with components held together by four O-H...N hydrogen bonds. In each case, the molecules assemble to form a discrete four-component assembly with olefins preorganized for a [2 + 2] photodimerization. UV irradiation of each member in the series of solids produces rctt-tetrakis(4-pyridyl)cyclobutane (4,4′-tpcb), stereospecifically, in up to 100% yield.
Structure/Activity relationships of Grandinol: a Germination Inhibitor in Eucalyptus
Bolte, Matthew L.,Crow, Wilfrid D.,Takahashi, Nobutaka,Sakurai, Akira,Uji-Ie, Masami,Yoshida, Shigeo
, p. 761 - 768 (2007/10/02)
Structure/activity relationships of grandinol (1), which shows potent inhibition to cress germination, were examined by an activity comparison of many synthetic analogues.The result clearly indicates that a combination of two carbonyl functionalities on a
