516491-68-2

Upstream product

• 516491-57-9 2-[(1-tert-butoxycarbonylamino-cyclopentanecarbonyl)-amino]-3-[6-(3-nitro-phenyl)-pyridin-3-yl]-propionic acid ethyl ester 
• 248924-63-2 2-(benzhydrylidene-amino)-3-[6-(3-nitro-phenyl)-pyridin-3-yl]-propionic acid ethyl ester 
• 248924-16-5 2-(benzhydrylidene-amino)-3-(6-bromo-pyridin-3-yl)-propionic acid ethyl ester 
• 101990-45-8 2-bromo-5-bromomethylpyridine 
• 76792-22-8 (R)-2-bromoisovaleric acid 

Downstream Products

• 248924-66-5 2-{[1-((S)-2-Acetylsulfanyl-3-methyl-butyrylamino)-cyclopentanecarbonyl]-amino}-3-[6-(3-nitro-phenyl)-pyridin-3-yl]-propionic acid ethyl ester 

Relevant academic research and scientific papers

Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1

Directed screening of metalloprotease inhibitors identified CGS 30084 (1) as a potent inhibitor of endothelin-converting enzyme-1 (ECE-1) in vitro (IC50=77 nM). Herein we report the syntheses and biological activities of analogues containing modified biphenyl moieties, bearing heterocyclic proximal rings. Compound 20, the thioacetate ethyl ester prodrug derivative of compound 19a, was found to be an orally active and potent inhibitor of ECE-1 activity in rats.