Author/Authors :
Jun Li، نويسنده , , Stephanie Y. Chen، نويسنده , , Shiwei Tao، نويسنده , , Haixia Wang، نويسنده , , James J. Li، نويسنده , , Steve Swartz، نويسنده , , Christa Musial، نويسنده , , Andres A. Hernandez، نويسنده , , Neil Flynn، نويسنده , , Brian J. Murphy، نويسنده , , Blake Beehler، نويسنده , , Kenneth E. Dickinson، نويسنده , , Leah Giupponi، نويسنده , , Gary Grover، نويسنده , , Ramakrishna Seethala، نويسنده , , Paul Sleph، نويسنده , , Dorothy Slusarchyk، نويسنده , , Mujing Yan، نويسنده , , William G. Humphreys، نويسنده , , Hongjian Zhang، نويسنده , , et al.، نويسنده ,
Abstract :
The structure–activity relationship of the O-benzyl serine side chain was investigated based on the tetrazole-based growth hormone secretagogue BMS-317180 (2). The ortho position of the benzyl moiety was found to be favorable for introduction of substituents. A series of ortho-substituted compounds were synthesized with improved in-vitro and in-vivo activity. Among them, the biphenyl compound 2p shows twofold improvement in potency compared to its parent compound BMS-317180 (2).
