2. Academic Validation
  3. Highly potent growth hormone secretagogues

Highly potent growth hormone secretagogues

  • Bioorg Med Chem Lett. 2007 Jul 1;17(13):3657-9. doi: 10.1016/j.bmcl.2007.04.050.
Zhijian Lu 1,  James R Tata,  Kang Cheng,  Liente Wei,  Wanda W-S Chan,  Bridget Butler,  Klaus D Schleim,  Thomas M Jacks,  Gerard Hickey,  Arthur A Patchett
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. [email protected]
PMID: 17482461 DOI: 10.1016/j.bmcl.2007.04.050
Abstract

During an effort to search for more potent growth hormone secretagogues, we discovered a class of compounds of which the best compound 8 was 7-fold more active in vitro than the best compound in the series we revealed before [Tata, J. R.; Lu, Z.; Jacks, T. M.; Schleim, K. D.; Cheng, K.; Wei, L.; Chan, W.-S.; Butler, B.; Tsou, N.; Leung, K.; Chiu, S.-H. L.; Hickey, G. J.; Smith, R. G.; Patchett, A. A. Bioorg. Med. Chem. Lett.1997, 7, 2319.]. Animal studies show that compound 8 can stimulate growth hormone release at the oral dose as low as 0.06 mpk. Chemistry and biological studies are discussed.

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