Synthesis of the non-peptidic snail toxin 6-bromo-2-mercaptotryptamine dimer (BrMT)(2), its lower and higher thio homologs and their ability to modulate potassium ion channels.
Bioorg Med Chem Lett
; 23(20): 5503-6, 2013 Oct 15.
Article
in En
| MEDLINE
| ID: mdl-24021461
ABSTRACT
The first synthesis of the non-peptidic snail toxin 6-bromo-2-mercaptotryptamine dimer (BrMT)2 is described, along with the preparation of its lower and higher thio homologs. The synthetic (BrMT)2 and its derivatives reported herein are all capable of slowing the activation of the Kv1.1 potassium ion channel. Only the monosulfide variant shows significant slowing of the deactivation process. This synthetic strategy can now be applied to creating a more extensive set of compounds that vary in the length of the linker connecting the two monomers, the substituents on the indole ring core, and terminal amine.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Toxins, Biological
/
Tryptamines
/
Potassium Channel Blockers
/
Kv1.1 Potassium Channel
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2013
Document type:
Article
Affiliation country: