1.
J Org Chem
; 74(11): 4354-6, 2009 Jun 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19397301
RESUMO
We report the synthesis of macrocycles 1-6 via ring closing metathesis of dienes 7-12. Addition of chlorodicyclohexylborane to thermal and microwave assisted RCM of dienes 8 and 9 markedly improves the yield. The geometric isomers of macrocycles 1-3 and 5 have been assigned using X-ray crystallography and NMR.
2.
Angew Chem Int Ed Engl
; 48(8): 1455-8, 2009.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19145612
RESUMO
The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacification in an ovine-lens culture assay and is a lead compound for the development of a drug for cataract treatment. Cbz=carbobenzyloxy.