Alkyl-substituted amino acid amides and analogous di-and triamines: new non-peptide G protein activators

C Leschke, R Storm, E Breitweg-Lehmann…

Index: Leschke, Christian; Storm, Ruediger; Breitweg-Lehmann, Evelyn; Exner, Torsten; Nuernberg, Bernd; Schunack, Walter Journal of Medicinal Chemistry, 1997 , vol. 40, # 19 p. 3130 - 3139

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Citation Number: 28

Abstract

Synthesis and pharmacological properties of new potent direct activators of heterotrimeric G proteins are described. Compounds were synthesized from protected amino acids with alkylamines using coupling reagents (CDI, DCC, and EDC). Alkyl-substituted amino acid amides and their corresponding di-and triamines were subjected to structure-activity analysis. All compounds activated membrane-bound HL-60 GTPases in a pertussis toxin- ...