58631-66-6

Upstream product

• 625-36-5 2-chloropropionyl chloride 
• 541-73-1 1,3-Dichlorobenzene 
• 1078572-36-7 1-(2,4-dichlorophenyl)-3-hydroxypropanone 

Downstream Products

• 62847-54-5 1-(2,4-dichloro-phenyl)-3-nitro-propan-1-one 
• 113696-85-8 1-Chloro-3-(2,4-dichloro-phenyl)-pentan-3-ol 
• 113720-99-3 1-(2,4-dichlorobenzoylethyl)-4-(3,4,5-trimethoxybenzyl)piperazine dihydrochloride 
• 1037716-75-8 1-(2,4-dichlorophenyl)-3-chloropropanol 
• 56045-66-0 3-chloro-5-(2,4-dichloro-phenyl)-isoxazole 
• 113696-67-6 1-<3-(2,4-dichlorophenyl)-3-hydroxypentyl>-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride 
• 113721-02-1 3-(2,4-Dichloro-phenyl)-1-[4-(3,4,5-trimethoxy-benzyl)-piperazin-1-yl]-hexan-3-ol; hydrochloride 

Relevant academic research and scientific papers

Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation

The ATP-gated P2X7 purinergic receptor (P2X7) is involved in the pathogenesis of many neurodegenerative diseases (NDDs). Several P2X7 antagonists have been developed, though none of them reached clinical trials for this indication. In this work, we designed and synthesized novel blood-brain barrier (BBB)-permeable derivatives as potential P2X7 antagonists. They comprise purine or xanthine cores linked to an aryl group through different short spacers. Compounds were tested in YO-PRO-1 uptake assays and intracellular calcium dynamics in a human P2X7-expressing HEK293 cell line, two-electrode voltage-clamp recordings in Xenopus laevis oocytes, and in interleukin 1β release assays in mouse peritoneal macrophages. BBB permeability was assessed by parallel artificial membrane permeability assays and P-glycoprotein ATPase activity. Dichloroarylpurinylethanones featured a certain P2X7 blockade, being compound 6 (2-(6-chloro-9H-purin-9-yl)-1-(2,4-dichlorophenyl)ethan-1-one), named ITH15004, the most potent, selective, and BBB-permeable antagonist. Compound 6 can be considered as a first non-nucleotide purine hit for future drug optimizations.

4-MEMBERED RING CARBOXAMIDES USED AS NEMATICIDES

Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.

1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies

New 1-[(3-aryloxy-3-aryl)propyl]-1H-imidazoles were synthesized and evaluated against Candida albicans and dermatophytes in order to develop structure-activity relationships (SARs). Against C. albicans the new imidazoles showed minimal inhibitory concentrations (MICs) comparable to those of ketoconazole, miconazole, and econazole, and were more potent than fluconazole. Several derivatives (10, 12, 14, 18-20, 24, 28, 29, 30, and 34) turned out to be potent inhibitors of C. albicans strains resistant to fluconazole, with MIC values less than 10 μg/mL. Against dermatophytes strains, compounds 20, 25, and 33 (MIC ≤ 5 μg/mL) were equipotent to ketoconazole, econazole, and miconazole. SARs of imidazoles 10-44 were rationalized with reasonable accuracy by a previously developed quantitative pharmacophore for antifungal agents.