| 18295486 |
Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P, Slusarchyk D, Yan M, Humphreys WG, Zhang H, Ewing WR, Robl JA, Gordon D, Tino JA: Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1825-9. Epub 2008 Feb 13.
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). |
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