Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

Vasudevan A; Souers AJ; Freeman JC; Verzal MK; Gao J; Mulhern MM; Wodka D; Lynch JK; Engstrom KM; Wagaw SH; Brodjian S; Dayton B; Falls DH; Bush E; Brune M; Shapiro RD; Marsh KC; Hernandez LE; Collins CA; Kym PR

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

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Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

机译：氨基哌啶吲唑类是口服有效的黑色素浓缩激素受体-1拮抗剂。

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The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.

机译：报道了新型3-氨基吲唑黑色素浓缩激素受体-1拮抗剂的合成和生物学评估，其中几种已证明其功能活性低于100nM。化合物19和28是这项研究中确定的两种更有效的化合物，其特征是在大脑中的暴露量很高，并且在饮食诱导的肥胖小鼠中给药时表现出强大的功效。

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《Bioorganic and Medicinal Chemistry Letters》 |2005年第23期|共5页
作者
Vasudevan A; Souers AJ; Freeman JC; Verzal MK; Gao J; Mulhern MM; Wodka D; Lynch JK; Engstrom KM; Wagaw SH; Brodjian S; Dayton B; Falls DH; Bush E; Brune M; Shapiro RD; Marsh KC; Hernandez LE; Collins CA; Kym PR;
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正文语种 eng
中图分类基础医学;
关键词
receptor; antagonists; melanin-concentrating hormone; novel; Evaluation;

机译：受体;拮抗剂;黑色素浓缩激素;小说;评价;

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1. Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists. [J] . Vasudevan A, Souers AJ, Freeman JC, Bioorganic and Medicinal Chemistry Letters . 2005,第23期

机译：氨基哌啶吲唑类是口服有效的黑色素浓缩激素受体-1拮抗剂。
2. Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists. [J] . Wu WL, Burnett DA, Caplen MA, Bioorganic and Medicinal Chemistry Letters . 2006,第14期

机译：设计和合成口服有效的苯并咪唑类药物，作为黑色素浓缩激素受体1拮抗剂。
3. Promising strategies for obesity pharmacotherapy: melanocortin-4 (MC-4) receptor agonists and melanin concentrating hormone (MCH) receptor-1 antagonists. [J] . Jeon MK, Cheon HG Current topics in medicinal chemistry . 2009,第6期

机译：肥胖药物治疗的有希望的策略：黑皮质素4（MC-4）受体激动剂和黑色素浓缩激素（MCH）受体1拮抗剂。
4. Efficient Synthesis of Disulfide Bridge Containing Peptides: Melanin Concentrating Hormone (MCH) and Brain Natriuretic Peptide (BNP) [C] . Jianjun Jiang, Brian D. Dayton, Sevan J. Brodjian American Peptide Symposium . 2006

机译：高效合成含有肽的二硫桥：黑色素浓缩激素（MCH）和脑利钠肽（BNP）
5. Appetite regulation in winter flounder (Pseudopleuronectes americanus): characterization of melanin-concentrating hormone (MCH) and gonadotropin-releasing hormone (GnRH) transcript families and their role in feeding behaviour. [D] . Tuziak, Sarah. 2011

机译：冬季比目鱼（Pseudopleuronectes americanus）的食欲调节：黑色素浓缩激素（MCH）和促性腺激素释放激素（GnRH）转录本家族的特征及其在喂养行为中的作用。
6. Preparation and First Preclinical Evaluation of 18FFE@SNAP: A Potential PET Tracer for the Melanin-Concentrating Hormone Receptor-1 (MCHR1) [O] . Cécile Philippe, Lukas Nics, Markus Zeilinger, 2013

机译：18F FE @ SNAP的制备和首次临床前评估：黑色素浓缩激素受体1（MCHR1）的潜在PET示踪剂。
7. Discovery of Orally Efficacious Melanin-Concentrating Hormone Receptor-1 Antagonists as Antiobesity Agents. Synthesis, SAR, and Biological Evaluation of Bicyclo3.1.0hexyl Ureas [O] . -1

机译：发现口服有效的黑色素浓缩激素受体-1拮抗剂作为抗菌剂。己基的合成，SAR和生物学评价3.1.0己基脲

Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

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