- Cantffln - 6 - quaternary ammonium salt and its preparation method and application
-
The invention relates to a canthium dicoccum-6-one quaternary ammonium salt and a preparation method and an application thereof. The structural formula of the compound is shown in a formula (1) in the specification, wherein R is ethyl, propyl, isopropyl, allyl, normal-butyl, isobutyl, normal-amyl, normal-octyl, unsubstituted benzyl or substituted benzyl substituted by a hydrogen atom, methyl, bromomethyl, trifluoromethyl, benzyloxyl, a fluorine atom or a chlorine atom; X is chlorine, bromine or iodine. The application is that of the compound for preparing antibacterial drugs.
- -
-
-
- Synthesis, in vitro antibacterial activities of a series of 3-N-substituted canthin-6-ones
-
An improved synthetic route of canthin-6-one was accomplished. To further enhance the antibacterial potency and improve water solubility, a series of 3-N-alkylated and 3-N-benzylated canthin-6-ones were designed and synthesized, and their in vitro antibacterial activities were evaluated. A clear structure-activity relationship with peak minimal inhibitory concentration (MIC) values of 0.98 (μg·mL-1) was investigated. Particularly, compounds 6i-r and 6t were found to be the most potent compounds with minimal inhibitory concentration (MIC) values lower than 1.95 (μg·mL-1) against Staphylococcus aureus.
- Dai, Jiang-Kun,Dan, Wen-Jia,Li, Na,Du, Hong-Tao,Zhang, Ji-Wen,Wang, Jun-Ru
-
p. 580 - 583
(2016/01/09)
-
- An improved synthesis of canthin-6-one
-
An improved route has been devised which provides canthin-6-one in the highest yield from tryptamine to date. Tryptamine is converted to Nb-benzyltryptamine via reaction with benzoylchloride and reduction using LAH. Pictet-Spengler condensation with 2-ketoglutaric acid, removal of the protecting group by CTH, and aromatization with MnO2 affords canthin-6-one in 48% overall yield.
- Czerwinski, Kevin M.,Zificsak, Craig A.,Stevens, John,Oberbeck, Melissa,Randlett, Christopher,King, Melissa,Mennen, Steve
-
p. 1225 - 1231
(2007/10/03)
-
- Bonafousine et isobonafousine, alcaloides dimeres de Bonafousina tetrastachya (Humbolt, Bonpland et Kunth) Markgraf (Appocynacees)
-
The isolation of two new dimeric indole alkaloids, extracted from the leaves of Bonafousia tetrastachya (Apocynaceae), bonafousine and isobonafousine, is described.Their structures are elucidated using mainly mass spectrometry and (13)C n.m.r. spectroscopy.
- Damak, Mohamed,Ahond, Alain,Potier, Pierre
-
p. 490 - 495
(2007/10/02)
-