The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency

B Peschke, M Ankersen, M Bauer, TK Hansen…

Index: Peschke, Bernd; Ankersen, Michael; Bauer, Michael; Hansen, Thomas Kruse; Hansen, Birgit Sehested; Nielsen, Karin Kramer; Raun, Kirsten; Richter, Lutz; Westergaard, Lisbet European Journal of Medicinal Chemistry, 2002 , vol. 37, # 6 p. 487 - 501

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Citation Number: 11

Abstract

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4- piperidinylamino-and 4-dimethylaminopiperidino-substitutents were found to give the most active compounds. A replacement of the 4-dimethylaminopiperidino-substituent with 4- ...