108534-47-0Relevant articles and documents
Isolation, synthesis, and biological activity of biphenyl and m-terphenyl-type compounds from Dictyostelium cellular slime molds
Kikuchi, Haruhisa,Matsuo, Yusuke,Katou, Yasuhiro,Kubohara, Yuzuru,Oshima, Yoshiteru
, p. 8884 - 8889 (2012)
From the fruiting bodies of Dictyostelium polycephalum, we obtained four aromatic compounds: dictyobiphenyl A (1) and B (2) and dictyoterphenyl A (3) and B (4). The synthesis of 1-4 was performed to confirm the structures and obtain sufficient material fo
Efficient preparation of apically substituted diamondoid derivatives
Kahl, Paul,Tkachenko, Boryslav A.,Novikovsky, Anatoliy A.,Becker, Jonathan,Dahl, Jeremy E. P.,Carlson, Robert M. K.,Fokin, Andrey A.,Schreiner, Peter R.
, p. 787 - 798 (2014)
We present an effective three-step chromatography-free sequence for the preparation of apical monohydroxy derivatives of diamantane, triamantane, and [121]tetramantane from the corresponding bis-apical diols utilizing tert-butyldimethylsilyl chloride as t
Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors
Song, Lijun,Merceron, Romain,Hulpia, Fabian,Lucía, Ainhoa,Gracia, Bego?a,Jian, Yanlin,Risseeuw, Martijn D.P.,Verstraelen, Toon,Cos, Paul,Aínsa, José A.,Boshoff, Helena I.,Munier-Lehmann, Hélène,Savvides, Savvas N.,Van Calenbergh, Serge
, (2021/08/27)
Mycobacterium tuberculosis thymidylate kinase (MtTMPK) has emerged as an attractive target for rational drug design. We recently investigated new families of non-nucleoside MtTMPK inhibitors in an effort to diversify MtTMPK inhibitor chemical space. We here report a new series of MtTMPK inhibitors by combining the Topliss scheme with rational drug design approaches, fueled by two co-crystal structures of MtTMPK in complex with developed inhibitors. These efforts furnished the most potent MtTMPK inhibitors in our assay, with two analogues displaying low micromolar MIC values against H37Rv Mtb. Prepared inhibitors address new sub-sites in the MtTMPK nucleotide binding pocket, thereby offering new insights into its druggability. We studied the role of efflux pumps as well as the impact of cell wall permeabilizers for selected compounds to potentially provide an explanation for the lack of correlation between potent enzyme inhibition and whole-cell activity.
Selective ether bond breaking method of aryl alkyl ether
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Paragraph 0273-0275, (2020/09/16)
The invention discloses a selective aryl alkyl ether cracking method, which comprises that aryl alkyl ether, aluminum iodide and an additive are subjected to a selective ether bond cleavage reaction in an organic solvent at a temperature of -20 DEG C to a reflux temperature to generate phenol and derivatives thereof. The method is mild in condition and simple and convenient to operate, is suitablefor cracking aryl alkyl ether containing o-hydroxyl and o-carbonyl and acetal ether, and can also be used for removing tertiary carbon hydroxyl protecting groups with higher steric hindrance, such astriphenylmethyl, tertiary butyl and the like.
