| 1207719-14-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• CAS: 1207719-14-9
• 化学式: C₄₄H₄₉N₇O₆
• 分子量: 771.916
• InChiKey: LEOHCRVAYKZDRP-UPMQVBECSA-N

反应信息

• 作为产物：
  描述：

  9-芴甲基-N-琥珀酰亚胺基碳酸酯 、 、 (4R)-methyl 2-[3-(9-fluorenylmethoxycarbonyl)-2,2-dioxo-1,2,3-oxathiazolidin-4-yl]acetate 在 N,O-双三甲硅基乙酰胺 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 生成 、
  参考文献：
  名称：

  Structure–Activity Analysis of the Growth Hormone Secretagogue GHRP-6 by α- and β-Amino γ-Lactam Positional Scanning

  摘要：

  Incorporation of amino lactams into biologically active peptides restricts conformational mobility and may enhance selectivity and increase potency. α‐ and β‐amino γ‐lactams (Agl and Bgl), in both S and R configurations, were introduced into the growth hormone secretagogue GHRP‐6 using a Fmoc‐compatible solid‐phase protocol relying on N‐alkylation with five‐ and six‐membered cyclic sulfamidates, followed by lactam annulation under microwave heating. Using this protocol in conjunction with IRORI KanTM techniques furnished eleven new GHRP‐6 analogs, and their binding affinity IC50 values on both the growth hormone secretagogue receptor 1a (GHS‐R1a) and CD36 receptors are herein reported. The results indicate that selectivity towards one receptor or the other can be modulated by lactam substitution, typically at the Ala3 and the d‐Phe5 positions.

  DOI：

  10.1111/j.1747-0285.2009.00913.x