40130-25-4Relevant articles and documents
Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker
Abdelhameed, Ahmed,Feng, Mei,Joice, April C.,Zywot, Emilia M.,Jin, Yiru,La Rosa, Chris,Liao, Xiaoping,Meeds, Heidi L.,Kim, Yena,Li, Junan,McElroy, Craig A.,Wang, Michael Zhuo,Werbovetz, Karl A.
, p. 1901 - 1922 (2021/02/22)
Due to the limitations of existing medications, there is a critical need for new drugs to treat visceral leishmaniasis. Since arylimidamides and antifungal azoles both show oral activity in murine visceral leishmaniasis models, a molecular hybridization approach was employed where arylimidamide and azole groups were separated by phenoxyalkyl linkers in an attempt to capitalize on the favorable antileishmanial properties of both series. Among the target compounds synthesized, a greater antileishmanial potency against intracellular Leishmania donovani was observed as the linker length increased from two to eight carbons and when an imidazole ring was employed as the terminal group compared to a 1,2,4-triazole group. Compound 24c (N-(4-((8-(1H-imidazol-1-yl)octyl)oxy)-2-isopropoxyphenyl) picolinimidamide) displayed activity against L. donovani intracellular amastigotes with an IC50 value of 0.53 μM. When tested in a murine visceral leishmaniasis model, compound 24c at a dose of 75 mg/kg/day p.o. for five consecutive days resulted in a modest 33% decrease in liver parasitemia compared to the control group, indicating that further optimization of these molecules is needed. While potent hybrid compounds bearing an imidazole terminal group were also strong inhibitors of recombinant CYP51 from L. donovani, as assessed by a fluorescence-based assay, additional targets are likely to play an important role in the antileishmanial action of these compounds.
A intermediate [...] 2-hydroxy-5-nitrophenetol preparation method (by machine translation)
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Paragraph 0024; 0025, (2016/10/20)
This invention has offered a kind of [...] intermediate 2-hydroxy-5-nitrophenetol preparation method, the specific method of operation: added to the reaction vessel and dichloroethane ortho-hydroxy phenetole, for 0 °C slow dropwise N 2 O 5-dichloroethane solution, adds Bi Yu 30-35 ° C reaction 1-2 hours after, adding water to the reaction solution, extracting the organic phase, the resulting organic phase is dried by anhydrous sodium sulfate, filtered, the solvent is distilled under reduced pressure to obtain the required 2-hydroxy-5-nitrophenetol. This invention adopts the N 2 O 5/C 2 H 4 Cl 2 solution for nitration reagent reaction is high in efficiency, less side reaction, no waste acid pollution, the significance of specific green the environment-friendly production, the resulting product 2-hydroxy-5-nitrophenetol purity as high as 97% or more, the yield is up to 95% or more, the preparation method of mild reaction conditions and the process is simple, easy to operate, is suitable for industrial production. (by machine translation)
Highly efficient catalytic nitration of phenolic compounds by nitric acid with a recoverable and reusable Zr or Hf oxychloride complex and KSF
Shi, Min,Cui, Shi-Cong,Yin, Wan-Po
, p. 2379 - 2384 (2007/10/03)
Phenolic compounds can be nitrated with 60% nitric acid (1.2 equiv.) in the presence of catalytic amounts of a Zr or Hf oxychloride complex and montmorillonite KSF to give the corresponding nitrated products in good yields in a heterogeneous catalytic system. The co-catalyst and montmorillon ite can be easily recovered and reused in the next batch of nitration. This is a practical process for the nitration of phenolic compounds in a clean way. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
