- Tentoxin as a scaffold for drug discovery. Total solid-phase synthesis of tentoxin and a library of analogues.
Tentoxin as a scaffold for drug discovery. Total solid-phase synthesis of tentoxin and a library of analogues.
Organic letters (2003-06-07)
Jose C Jiménez, Bibiana Chavarría, Angel López-Macià, Miriam Royo, Ernest Giralt, Fernando Albericio
PMID12790542
RESUMO
[reaction: see text] A solid-phase method for the synthesis of tentoxin has been developed. Two key steps-dehydration and N-alkylation-are carried out while the peptide is anchored to the resin. The method, which has been validated by the preparation of a library of tentoxin analogues, should be applicable to the generation of further libraries that have the tentoxin scaffold structure, as well as other structures containing N-alkylated didehydroamino acids.
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Tentoxin from Alternaria tenuis, Naturally occurring phytotoxic cyclic tetrapeptide