Author/Authors :
Jun Li، نويسنده , , Stephanie Y. Chen، نويسنده , , Brian J. Murphy، نويسنده , , Neil Flynn، نويسنده , , Ramakrishna Seethala، نويسنده , , Dorothy Slusarchyk، نويسنده , , Mujing Yan، نويسنده , , Paul Sleph، نويسنده , , Hongjian Zhang، نويسنده , , William G. Humphreys، نويسنده , , William R. Ewing، نويسنده , , Jeffrey A. Robl، نويسنده , , David Gordon، نويسنده , , Joseph A. Tino، نويسنده ,
Abstract :
The first enantioselective synthesis of (d)-2-tert-butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid 3 was achieved. The incorporation of the titled compound into growth hormone secretagogue (GHS) compounds resulted in new analogs 10 and 16, both of which had significantly increased in vitro potency. The compound 10 also showed improved in vivo efficacy as well as pharmacokinetic properties in rat models.
