Synthesis and biological activities of phenyl piperazine- based peptidomimetic growth hormone secretagogues

https://doi.org/10.1016/S0960-894X(98)00238-8Get rights and content

Abstract

A new class of potent, orally active phenyl piperazine-based GH secretagogues have been discovered from attempts to mimic the arrangement of the phenyl substitutent in the spiroindanyl piperidine and spiroindoline sulfonamide privileged structures of 4 and 1, respectively. The best of these compounds, 18 (EC50 = 2.8 nM) is nearly as potent as MK-0677 for releasing GH from rat pituitary cells.

A new class of potent orally active phenyl piperazine-based GH secretagougues such as compound 17 (L-163,689, EC50 = 6.3 mM) have been discovered from attempts to mimic the arrangement of the phenyl substituent in the spiroindanyl piperidine and spiroindoline sulfonamide privileged structures of 4 and 1, respectively.

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