24155-46-2

Upstream product

• 24155-33-7 1-(4-fluorophenyl)-2-(1H-imidazol-1-yl)ethanone 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 403-29-2 2-bromo-4'-fluoroacetophenone 

Downstream Products

• 223760-54-1 methyl (2S)-2-{4-[1-(4-fluorophenyl)-2-(imidazol-1-yl)ethoxy]-2-(4-fluorophenyl)benzoylamino}-4-methylsulfanylbultyrate 
• 223760-77-8 methyl 5-[1-(4-fluorophenyl)-2-(imidazol-1-yl)ethoxy]-2-(4-fluorophenethyl)benzoate 
• 223760-87-0 methyl 4-[2-(imidazol-1-yl)-1-(4-fluorophenyl)ethoxy]-2-(4-fluorophenyl)benzoate 
• 223761-01-1 methyl 2-(4-fluorophenyl)-6-[1-(4-fluorophenyl)-2-(imidazol-1-yl)ethoxy]pyridin-3-carboxylate 
• 223759-38-4 methyl (2S)-2-{2-phenyl-4-[1-(4-fluorophenyl)-2-(imidazol-1-yl)ethoxymethyl]benzoylamino}-4-methylsulfanylbutyrate 
• 223760-55-2 methyl 2-(4-fluorophenyl)-4-[2-(imidazol-1-yl)-1-(4-fluorophenyl)ethoxymethyl]benzoate 
• 223760-29-0 methyl (2S)-2-{2-(4-fluorophenethyl)-5-[2-(imidazol-1-yl)-1-(4-fluorophenyl)-ethoxymethyl]benzoylamino}-4-methylsulfanyl butyrate 
• 223760-30-3 methyl (2S)-2-{2-(4-fluorobenzyl)-5-[1-(4-fluorophenyl)-2-(imidazol-1-yl)ethoxymethyl]benzoylamino}-4-methylsulfanylbutyrate 
• 1363792-18-0 1-(4-fluorophenyl)-2-(1H-imidazol-1-yl)ethyl [4-(propan-2-yl)phenyl]carbamate 
• 1363792-08-8 (+/-)-1-(4-fluorophenyl)-2-(1H-imidazol-1-yl)ethyl 3-(trifluoromethyl)benzoate 
• 1363792-12-4 (+/-)-1-(4-fluorophenyl)-2-(1H-imidazol-1-yl)ethyl biphenyl-4-carboxylate 
• 1363792-15-7 1-(4-fluorophenyl)-2-(1H-imidazol-1-yl)ethyl phenoxyacetate 
• 1620488-60-9 1-(4-fluorophenyl)-2-imidazol-1-yl-ethyl 4-(3-nitro-2-pyridyl)piperazine-1-carboxylate 
• 1620488-64-3 1-(4-fluorophenyl)-2-imidazol-1-yl-ethyl 4-(4-nitrophenyl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

Novel BuChE-IDO1 inhibitors from sertaconazole: Virtual screening, chemical optimization and molecular modeling studies

In our effort towards the identification of novel BuChE-IDO1 dual-targeted inhibitor for the treatment of Alzheimer's disease (AD), sertaconazole was identified through a combination of structure-based virtual screening followed by MM-GBSA rescoring. Preliminary chemical optimization was performed to develop more potent and selective sertaconazole analogues. In consideration of the selectivity and the inhibitory activity against target proteins, compounds 5c and 5d were selected for the next study. Further modification of compound 5c led to the generation of compound 10g with notably improved selectivity towards BuChE versus AChE. The present study provided us with a good starting point to further design potent and selective BuChE-IDO1 inhibitors, which may benefit the treatment of late stage AD.

BuChE-IDO1 inhibitor as well as preparation method and application thereof

The invention relates to the field of medicines, and particularly discloses a BuChE-IDO1 inhibitor as well as a preparation method and application thereof. The 7-chlorine-3-substituted benzothiophene part of sertaconazole is chemically modified, the influence of the 7-chlorine-3-substituted benzothiophene part of sertaconazole on the in-vitro inhibitory activity of AChE, BuChE and IDO1 is explored, the target compound is further optimized, and the technical problems that an existing BuChE-IDO1 inhibitor is poor in pertinence and safety are solved. What is explored is that an appropriate substituent group introduced to a 2-benzothiazole ring can form additional interaction with surrounding amino acids and heme iron, so that the binding affinity of the analogue with BuChE and IDO1 is increased, and a new idea is broadened for more efficient and targeted treatment of advanced AD diseases.

Diaryl-containing imidazole compound and preparation method and medical application thereof

The invention discloses a diaryl-containing imidazole compound. The invention further discloses application of the diaryl-containing imidazole compound to preparation of drugs for preventing or treating Alzheimer's disease. The inventor screens butyrylcholine esterase and IDO1 as carriers for inhibiting the activity to evaluate the effect of the diaryl imidazole compound to treat Alzheimer's disease, and finds that the diaryl imidazole compound has good in vitro activity, and can be further developed as a precursor substance for performing the Alzheimer's disease resistant effect by inhibitingthe activity of cholinesterase. (The formula is shown in the description).

Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)- 1-phenylethanol derivatives

A new series of aromatic ester and carbamate derivatives of 2-(1H-imidazol-1-yl)-1-phenylethanol were synthesized and evaluated for their antifungal activity towards Candida albicans and non-albicans Candida species strains. The aromatic biphenyl ester derivatives 6a-c were more active than the reference compound fluconazole. 6c possesses a MIC mean values of 1.7 ± 1.4 μg mL-1 vs C. albicans and 1.9 ± 2.0 μg mL -1 vs non-albicans Candida species strains. The racemic mixtures of 6a, b were purified to afford the pure enantiomers. The (-) isomers were up to 500 times more active than (+) isomers. (-)-6a and (-)-6b were thirty and ninety times more active than fluconazole towards C. krusei strain respectively. The racemates of 6a-c showed low cytotoxicity against human monocytic cell line (U937) with 6a demonstrating a CC50 greater than 128 μg mL -1.

Research on antibacterial and antifungal agents. X. Synthesis and antimicrobial activities of 1-phenyl-2-(1H-azol-1-yl) ethane derivatives. Anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl) ethanol.

The synthesis and antimicrobial activity of new phenylazolylethane derivatives are reported.Antimicrobial data in comparison with those obtained with miconazole, fluconazole, enilconazole, imazalil sulfate, pipemidic acid and minocycline showed that tested compounds generally possessed poor or weak activity.Toxicity and anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl)ethanol and structural likeness to Denzimol were also tested.The obtained results showed interesting anticonvulsant activity but only on the supraspinal region. azoles / antifungal / anticonvulsant agent