Synthesis and biological evaluation of nonpeptide mimetics of ω-conotoxin GVIA

…, SA Forsyth, RJ Lewis, YP Lok, CI Schroeder

Index: Baell, Jonathan B.; Duggan, Peter J.; Forsyth, Stewart A.; Lewis, Richard J.; Lok, Y. Phei; Schroeder, Christina I. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 15 p. 4025 - 4037

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Citation Number: 53

Abstract

A benzothiazole-derived compound (4a) designed to mimic the Cα–Cβ bond vectors and terminal functionalities of Lys2, Tyr13 and Arg17 in ω-conotoxin GVIA was synthesised, together with analogues (4b–d), which had each side-chain mimic systematically truncated or eliminated. The affinity of these compounds for rat brain N-type and P/Q-type voltage gated calcium channels (VGCCs) was determined. In terms of N-type channel affinity and ...