Synthesis and biological evaluation of destruxin A and related analogs.
J Pept Res
; 58(1): 1-11, 2001 Jul.
Article
em En
| MEDLINE
| ID: mdl-11454164
ABSTRACT
This report describes the development of an efficient solid-phase synthesis protocol and adaptation of reported solution phase procedures for the synthesis of the cyclic depsihexapeptide destruxin A and related analogs. The solid-phase method described is based on standard Fmoc peptide chemistry, including a new synthetic method for the assembly of the depsi bond-containing unit. In order to select analogs of destruxin A for synthesis and evaluation of insecticidal activity, the work of Hellberg et al., describing a set of Z-descriptors for amino acid side-chains comparing their physicochemical properties, was utilized. Destruxin A and 27 different analogs with structural variations in four residues were synthesized and insecticidal activity was evaluated via injections into tobacco budworm (Heliothis virescens) larvae. Several destruxin A analogs were found to be at least as potent as the native compound.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos Cíclicos
/
Bioquímica
/
Depsipeptídeos
/
Inseticidas
Limite:
Animals
Idioma:
En
Revista:
J Pept Res
Assunto da revista:
BIOQUIMICA
Ano de publicação:
2001
Tipo de documento:
Article
País de afiliação:
Alemanha
País de publicação:
DENMARK
/
DINAMARCA
/
DK