N G-Acyl-argininamides as NPY Y 1 receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity

S Weiss, M Keller, G Bernhardt, A Buschauer…

Index: Weiss, Stefan; Keller, Max; Bernhardt, Guenther; Buschauer, Armin; Koenig, Burkhard Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 17 p. 6292 - 6304

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Citation Number: 24

Abstract

NG-Acylated argininamides, covering a broad range of lipophilicity (calculated logD values:− 1.8–12.5), were synthesized and investigated for NPY Y1 receptor (Y1R) antagonism, Y1R affinity and stability in buffer (NG-deacylation, yielding BIBP 3226). Broad structural variation of substituents was tolerated. The Ki (binding) and Kb values (Y1R antagonism) varied from low nM to one-digit μM. Most of the compounds proved to be ...