Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

Sebhat IK; Lai Y; Barakat K; Ye Z; Tang R; Kalyani RN; Vongs A; Macneil T; Weinberg DH; Cabello MA; Maroto M; Teran A; Fong TM; Van-der-Ploeg LH; Patchett AA; Nargund RP

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Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

机译：黑皮质素亚型4受体激动剂：关于4-烷基哌啶核心的结构-活性关系。

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摘要

SAR about the piperidine core in a series of MC4R agonists is described. A number of alkyl substituents that furnish compounds with good affinity and functional potency are reported.

机译：描述了一系列MC4R激动剂中关于哌啶核心的SAR。据报道，许多烷基取代基可以提供具有良好亲和力和功能性的化合物。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2007年第20期|共4页
作者
Sebhat IK; Lai Y; Barakat K; Ye Z; Tang R; Kalyani RN; Vongs A; Macneil T; Weinberg DH; Cabello MA; Maroto M; Teran A; Fong TM; Van-der-Ploeg LH; Patchett AA; Nargund RP;
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正文语种 eng
中图分类药学;生物化学;
关键词
agonists; piperidine; structure; receptor;

机译：激动剂;哌啶;结构;受体;

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专利

1. Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core. [J] . Sebhat IK, Lai Y, Barakat K, Bioorganic and Medicinal Chemistry Letters . 2007,第20期

机译：黑皮质素亚型4受体激动剂：关于4-烷基哌啶核心的结构-活性关系。
2. Synthesis and Structure-Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor [J] . Timothy I. Richardson, Paul L. Ornstein, Karin Briner, Journal of Medicinal Chemistry . 2004,第3期

机译：新型芳香基哌嗪作为黑皮质素亚型4受体的有效激动剂和选择性激动剂的合成与构效关系
3. Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor [J] . Ericson Mark D., Freeman Katie T., Schnell Sathya M., Journal of Medicinal Chemistry . 2017,第19期

机译：宏环agouti相关蛋白（AgrP）支架的结构 - 活性关系研究显示agouti信号蛋白（ASP）残留物拮抗剂拮抗剂效力维持Melanocortin-4受体拮抗剂效力并导致Melanocortin-5受体的反向激动剂药理学
4. Structure-activity relationship studies of new cyclic MSH analogues using cloned-human melanocortin receptors lead to greater selectivity and inverse agonists [C] . Minying Cai, Paolo Grieco, Jonathan Wiens, the International Peptide Symposium . 2001

机译：使用克隆人黑素激素受体的新循环MSH类似物的结构 - 活性关系研究导致更大的选择性和反向激动剂
5. Selective GLP-1 receptor antagonists and glucagon/GLP-1 co-agonists discovered through an investigation into the structure-activity relationship in glucagon-related peptides. [D] . Patterson, James T. 2011

机译：通过研究胰高血糖素相关肽的结构-活性关系，发现了选择性的GLP-1受体拮抗剂和胰高血糖素/ GLP-1共激动剂。
6. Structure-Activity Relationships of Peptides Incorporating a Bioactive Reverse-Turn Heterocycle at the Melanocortin Receptors: Identification of a 5800-fold Mouse Melanocortin-3 Receptor (mMC3R) Selective Antagonist/Partial Agonist versus the Mouse Melanocortin-4 Receptor (mMC4R) [O] . Anamika Singh, Marvin Dirain, Rachel Witek, -1

机译：在Melanocortin受体上掺入生物逆向杂环的肽的结构-活性关系：鉴定为5800倍小鼠Melanocortin-3受体（mMC3R）选择性拮抗剂/部分激动剂与小鼠Melanocortin-4受体（mMC4R）
7. Synthesis and Structure-Activity Relationships of Novel Aryl Piperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor [O] . -1

机译：新型芳基哌嗪的合成与结构 - 活性关系作为黑素旋蛋白亚型-4受体的有效和选择性激动剂
8. Structure-Activity Relationships of 33 Piperidines as Toxicants Against Female Adults of Aedes aegypti (Diptera: Culicidae) [R] . Prodgeon, J. W., Meepagala, K. M., Becnel, J. J., 2007

机译：33种哌啶类作为对埃及伊蚊雌性成虫毒性的构效关系（双翅目：蚊科）

Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

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