30291-41-9Relevant articles and documents
Capsidone artificial hapten, artificial antigen and preparation method and application thereof
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Paragraph 0080-0083; 0099-0103; 0116-0120, (2020/08/09)
The invention relates to the field of cathinone artificial antigen structures, and particularly relates to a cathinone artificial antigen, an artificial antigen as well as a preparation method and application thereof. The cathinone artificial antigen is characterized in that a molecular structural formula of the cathinone artificial antigen is shown as follows: the formula (1) is shown in the description. According to the cathinone artificial antigen provided by the invention, a connecting arm is introduced onto a site N of cathinone, and the connecting arm is introduced onto the decoration site so that a characteristic structure of the cathinone is kept to a maximum extent; moreover, the cathinone artificial antigen has an active group coupled with carrier protein and can be used as an antigen determinant group. Compared with an annular connecting arm, the connecting arm adopted by the invention is chain-shaped, an identification degree of T cells to the connecting arm can be reducedas much as possible during immunization, so that an antibody obtained by immunization has higher specificity and affinity to the cathinone.
Novel derivatives of substituted 6-fluorobenzothiazole diamides: synthesis, antifungal activity and cytotoxicity
Pejchalová, Marcela,Havelek, Radim,Královec, Karel,R??i?ková, Zdeňka,Pejchal, Vladimír
, p. 1847 - 1862 (2017/08/03)
A new series of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-substituted phenyl diamides were synthesized in vitro as potential antifungal agents. Chemical structures of the synthesised compounds were substantiated by IR, 1H, 13C, 19F nuclear magnetic resonance spectra, high resolution mass spectrometry, elemental analysis and also by X-ray diffraction. In addition, the cytotoxicity of the most active compounds was investigated against cancer cell line (Jurkat) and one type of normal lung fibroblast cells (MRC-5) by (2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) tetrazolium salt reduction assay, propidium iodide flow cytometry assay and xCELLigence system allowing a label-free assessment of the cells proliferation. Compounds indicated as 11e, 11g, 11j, 11n and 11o, were the best of the series, showing minimum inhibitory concentration values of 6.25–50 μg/mL against pathogenic strains Candida albicans HE 169, Candida tropicalis 31/HK and Candida parapsilosis p69. Moreover compounds 11e, 11g, 11j and 11o did not show any cytotoxic effect against human Jurkat and MRC-5 cells.
Synthesis of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-substituted phenyl ureas and their inhibition activity to acetylcholinesterase and butyrylcholinesterase
Pejchal, Vladimir,Stepankova, Sarka,Drabina, Pavel
scheme or table, p. 57 - 62 (2011/03/21)
A series of novel 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3- substituted phenyl ureas were synthesized by the condensation of (1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethanamine with substituted phenyl isocyanates under mild conditions. Their structures were confirmed 1H, 13C, and 19F NMR spectra, and elemental analyses. The optical activities were confirmed by optical rotation measurements. The inhibition activity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2- yl)ethyl]-3-substituted phenyl ureas to acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) was also tested. Preliminary bioassay indicated that the target ureas displayed excellent acetylcholinesterase and butyrylcholinesterase inhibition activity.