A potent, orally bioavailable benzazepinone growth hormone secretagogue

RJ DeVita, R Bochis, AJ Frontier, A Kotliar…

文献索引：DeVita, Robert J.; Bochis, Richard; Frontier, Alison J.; Kotliar, Andrew; Fisher, Michael H.; Schoen, William R.; Wyvratt, Matthew J.; Cheng, Kang; Chan, Wanda W.-S.; Butler, Bridget; Jacks, Thomas M.; Hickey, Gerard J.; Schleim, Klaus D.; Leung, Kwan; Chen, Zhesheng; Lee Chiu; Feeney, William P.; Cunningham, Paul K.; Smith, Roy G. Journal of Medicinal Chemistry, 1998 , vol. 41, # 10 p. 1716 - 1728

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被引用次数: 46

摘要

The identification of L-739,943 (8b), a potent, orally bioavailable benzolactam growth hormone secretagogue, is obtained from zwitterionic L-692,429 through modification of its amino acid side chain and replacement of the acidic 2'-tetrazole with the neutral and potency enhancing 2'-(N-methylaminocarbonylamino) methyl substituent. L-739,943 is orally active for the release of growth hormone in beagle dogs at doses as low as 0.5 mg/kg. ...