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Synthesis and biological evaluation of anthranilamide-based non-peptide mimetics of ω-conotoxin GVIA
Jonathan B. Baell Peter J. Duggan Stewart A. Forsyth Y. Phei Lok Christina I. Schroeder 《Tetrahedron》2006,62(31):7284-7292
Non-peptide mimetics based on an anthranilamide ‘scaffold’ possessing fragments that mimic Lys2, Tyr13 and Arg17 in ω-conotoxin GVIA have been prepared. Compounds were assayed for binding to the voltage-gated calcium channels Cav2.2 (‘N-type’) and Cav2.1 (‘P/Q-type’) in rat brain. The primary synthetic target, 2-(6-amino-hexanoylamino)-5-(3-guanidino-propoxy)-N-[4-(4-hydroxyphenoxy)-phenyl]-benzamide (2a), exhibited low μM binding to Cav2.2 and was more than 30-fold selective for Cav2.2 over Cav2.1. 相似文献