64635-54-7Relevant academic research and scientific papers
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.
Production method of 3-ethoxy-4-nitrophenol
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Paragraph 0037, (2017/05/26)
The invention discloses a production method of 3-ethoxy-4-nitrophenol. The low-price m-dichlorobenzene is used instead of the high-price resorcinol as the raw material, and the methoxy is converted into the hydroxy; and a simple alkaline process is used instead of the conventional hydrogen bromide/acetic acid system to prepare the 3-ethoxy-4-nitrophenol. By using low-price m-dichlorobenzene instead of the high-price resorcinol as the raw material to prepare the 3-ethoxy-4-nitrophenol, the method has the advantages of simple synthesis steps, low pollution, environment friendliness, high product quality, high yield, low production cost and normal-pressure operation, and can implement industrial production.
