Liquid-phase combinatorial synthesis of 1,4-benzodiazepine-2,5-diones as the candidates of endothelin receptor antagonism.
Ming-Fu Cheng, Jim-Min Fang
Index: J. Comb. Chem. 6(1) , 99-104, (2004)
Full Text: HTML
Abstract
A library of 1,4-benzodiazepine-2,5-dione dicarboxylate derivatives containing aryl substituents at N(1)- and N(4)-positions to mimic the amino acid residues of Try-13, Phe-14, and Asp-18 in endothelin-1 is established by using the starting materials of alpha-amino esters, hydroxybenzaldehydes, nitrobenzoyl chlorides, and benzyl bromides in a polyethylene resin-bound liquid-phase synthesis. All of the six synthetic steps are conducted under mild conditions to give the desired products with reasonable yields and purity. The poly(ethylene glycol) support plays as a part of ester linkage that is released at the final step.
Related Compounds
Related Articles:
2003-10-01
[J. Food Prot. 66(10) , 1811-21, (2003)]
A Structure-Based Activation Model of Phenol-Receptor Protein Interactions. Lee K.
[Bull. Korean Chem. Soc. 18 , 16-22, (1997)]
4-Hydroxy-2, 6-dimethoxybenzaldehyde. Wuyts C, et al.
[Acta Crystallogr. Sect. E Struct. Rep. Online 61(1) , 79-80, (2004)]