3622-23-9Relevant articles and documents
Preparation method of 2,6'-dichlorobenzothiazole
-
Paragraph 0014-0025, (2019/08/30)
The invention discloses a preparation method of 2,6'-dichlorobenzothiazole, and belongs to the technical field of organic chemistry. The method comprises the following steps: using 2-amino-6-chlorobenzothiazole as a raw material and acetonitrile as a solvent, adding copper chloride and isoamyl nitrite, carrying out a reaction to form a mixture of 2,6'-dichlorobenzothiazole and other impurities, and carrying out column chromatography separation to obtain pure 2,6'-dichlorobenzothiazole at a yield of 45-66%. The preparation method makes up for the deficiency of existing synthesis processes, andprovides a new method for synthesizing the 2,6'-dichlorobenzothiazole.
Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles
Stella, Alessandro,Segers, Kenneth,De Jonghe, Steven,Vanderhoydonck, Bart,Rozenski, Jef,Anne, Jozef,Herdewijn, Piet
experimental part, p. 253 - 265 (2011/09/30)
The 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazole scaffold was selected as a central core structure for the discovery of novel antibacterial compounds. A systematic variation of the substituents on the oxo-pyrazole moiety, as well as on the benzo moiety, led to the creation of a small and focused library of benzothiazoles that was subjected to antibacterial screening. In a first round of screening, activity of the compounds against six representative microorganisms was established. For the most potent congeners, MIC values against S. aureus and P. aeruginosa were determined. The structure-activity relationship study clearly revealed that subtle structural variations influence the antibacterial activity to a large extent. The most potent congeners displayed MIC values of 3.30 μM.
Ferulic acid and benzothiazole dimer derivatives with high binding affinity to β-amyloid fibrils
Byeon, Seong Rim,Jin, Yun Jung,Lim, Soo Jeong,Lee, Ji Hoon,Yoo, Kyung Ho,Shin, Kye Jung,Oh, Seung Jun,Kim, Dong Jin
, p. 4022 - 4025 (2008/02/07)
New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [125I]TZDM for their specific binding affinities to Aβ fibrils. In particular, 4a showed the most excellent binding affinity (Ki = 0.53 nM), compared to PIB (Ki = 0.77 nM), for benzothiazole binding sites of Aβ1-42 fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of Aβ fibrils.