Synthesis, structure–property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y 12 receptor

…, RD Groneberg, DM Harvey, M O'Sullivan…

Index: Bach, Peter; Bostroem, Jonas; Brickmann, Kay; Van Giezen; Groneberg, Robert D.; Harvey, Darren M.; O'Sullivan, Michael; Zetterberg, Fredrik European Journal of Medicinal Chemistry, 2013 , vol. 65, p. 360 - 375

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Citation Number: 19

Abstract

Abstract The present paper describes the development of a new series of P2Y 12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC 50 binding affinity= 0.33 μM, aq solubility< 0.1 μM, microsomal CLint (HLM)≥ 300 μM/min/mg). By replacement of the urea functionality with a sulfonylurea group we observed increased affinity along with improved stability and solubility as exemplified by 47 (IC 50 binding ...