1009-06-9Relevant articles and documents
BENZIMIDAZOLE COMPOUNDS AS HDAC6 INHIBITORS
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, (2022/02/27)
Novel compounds of Formula I are described, where the compounds are selective HDAC6 inhibitors suitable for treatment of diseases associated with HDAC6, where X, Y, Z, A1, A2, Q1 and Q2 are as described.
Synthesis and antileishmanial activity of fluorinated rhodacyanine analogues: The ‘fluorine-walk’ analysis
Lasing, Thitiya,Phumee, Atchara,Siriyasatien, Padet,Chitchak, Kantima,Vanalabhpatana, Parichatr,Mak, Kit-Kay,Hee Ng, Chew,Vilaivan, Tirayut,Khotavivattana, Tanatorn
supporting information, (2019/12/09)
In a search for potent antileishmanial drug candidates, eighteen rhodacyanine analogues bearing fluorine or perfluoroalkyl substituents at various positions were synthesized. These compounds were tested for their inhibitory activities against Leishmania martiniquensis and L. orientalis. This ‘fluorine-walk’ analysis revealed that the introduction of fluorine atom at C-5, 6, 5′, or 6′ on the benzothiazole units led to significant enhancement of the activity, correlating with the less negative reduction potentials of the fluorinated analogues confirmed by the electrochemical study. On the other hand, [sbnd]CF3 and [sbnd]OCF3 groups were found to have detrimental effects, which agreed with the poor aqueous solubility predicted by the in silico ADMET analysis. In addition, some of the analogues including the difluorinated species showed exceptional potency against the promastigote and axenic amastigote stages (IC50 = 40–85 nM), with the activities surpassing both amphotericin B and miltefosine.
Synthesis method and intermediate for 2-bromo-5-fluoro-4-nitroaniline
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, (2020/01/12)
The invention discloses a synthesis method and an intermediate for 2-bromo-5-fluoro-4-nitroaniline. The synthesis method for 2-bromo-5-fluoro-4-nitroaniline comprises the step of carrying out a nitration reaction on 2-bromo-5-fluoroaniline and a nitration reagent to generate the 2-bromo-5-fluoro-4-nitroaniline, or comprises the following steps: reacting the 2-bromo-5-fluoroaniline with an amino protection reagent to obtain amino-protected 2-bromo-5-fluoroaniline, then carrying out the nitration reaction on the amino-protected 2-bromo-5-fluoroaniline and the nitration reagent to generate a nitration product that is the intermediate, and finally, removing the amino protection group from the nitration product to obtain the 2-bromo-5-fluoro-4-nitroaniline. The synthesis method has the advantages of high reaction yield, high product purity and easily available raw materials.