210364-77-5

Basic information

• Product Name: 1H-1,2,4-Triazole, 1-[2-(4-nitrophenoxy)ethyl]-
• Synonyms: 1-(2-{4-nitrophenoxy}ethyl)-1H-1,2,4-triazole
• CAS NO: 210364-77-5
• Molecular Formula: C₁₀H₁₀N₄O₃
• Molecular Weight: 234.2114
• Mol File: 210364-77-5.mol
• Article Data: 4

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 1H-1,2,4-Triazole, 1-[2-(4-nitrophenoxy)ethyl]-(CAS DataBase Reference)
• NIST Chemistry Reference: 1H-1,2,4-Triazole, 1-[2-(4-nitrophenoxy)ethyl]-(210364-77-5)
• EPA Substance Registry System: 1H-1,2,4-Triazole, 1-[2-(4-nitrophenoxy)ethyl]-(210364-77-5)

Safety Data

• Hazardous Substances Data: 210364-77-5(Hazardous Substances Data)

Upstream product

• 3383-72-0 1-(2-chloroethoxy)-4-nitrobenzene 
• 41253-21-8 sodium triazole 
• 288-88-0 1,2,4-Triazole 
• 16365-27-8 2-(4-nitrophenoxy)ethanol 
• 100-02-7 4-nitro-phenol 
• 13288-06-7 1-(2-bromoethoxy)-4-nitrobenzene 
• 350-46-9 4-Fluoronitrobenzene 

Downstream Products

• 314268-42-3 4-(2-(1H-1,2,4-triazol-1-yl)ethoxy)aniline 

Relevant articles and documents

Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker

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.

BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE

The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.