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• W1969574505 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′). These studies unexpectedly revealed quite a flat nanomolar/subnanomolar SAR for the binding affinity, while differences were seen in the in vitro functional activities. We propose that variations in the residence time may explain these results." @default.
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• W1969574505 date "2012-03-01" @default.
• W1969574505 modified "2023-10-03" @default.
• W1969574505 title "Design and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. Synthesis and structure-relationships of α,α-tetrahydropyranylglycine" @default.
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• W1969574505 doi "https://doi.org/10.1016/j.bmc.2012.01.036" @default.
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