Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. Synthesis and structure-relationships of α, α-tetrahydropyranylglycine

CI Fincham, A Bressan, P D'Andrea, A Ettorre…

Index: Fincham, Christopher I.; Bressan, Alessandro; D'Andrea, Piero; Ettorre, Alessandro; Giuliani, Sandro; Mauro, Sandro; Meini, Stefania; Paris, Marielle; Quartara, Laura; Rossi, Cristina; Squarcia, Antonella; Valenti, Claudio; Daniela, Fattori; Maggi, Carlo Alberto Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 6 p. 2091 - 2100

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Abstract

A series of α, α-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B2 (hB2) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity of a further evolution of the series, consisting in compounds of the general formula 2, containing either an alkyl piperazine or a 4-alkyl piperidine ring bearing various positively charged groups (R′). ...