Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists.

Guo L; Ye Z; Liu J; He S; Bakshi RK; Sebhat IK; Dobbelaar PH; Hong Q; Jian T; Dellureficio JP; Tsou NN; Ball RG; Weinberg DH; MacNeil T; Tang R; Tamvakopoulos C; Peng Q; Chen HY; Chen AS; Martin WJ; MacIntyre DE; Strack AM; Fong TM; Wyvratt MJ; Nargund RP

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists.

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Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists.

机译：发现有效，选择性和口服生物可利用的3H-螺螺（Isobenzofuran-1,4'-哌啶）的基于Melanocortin亚型-4受体激动剂。

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摘要

Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed.

机译：公开了一种基于3H-Spiro [Isobenzofuran-1,4'-哌啶]化合物的设计，合成和SAR作为有效的选择性和口服生物可利用的黑色主义素亚型-4受体（MC4R）激动剂。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第16期|共6页
作者
Guo L; Ye Z; Liu J; He S; Bakshi RK; Sebhat IK; Dobbelaar PH; Hong Q; Jian T; Dellureficio JP; Tsou NN; Ball RG; Weinberg DH; MacNeil T; Tang R; Tamvakopoulos C; Peng Q; Chen HY; Chen AS; Martin WJ; MacIntyre DE; Strack AM; Fong TM; Wyvratt MJ; Nargund RP;
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Department of Medicinal Chemistry Merck Research Laboratories PO Box 2000 Rahway NJ 07065 USA.;

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正文语种 eng
中图分类药学;生物化学;
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1. Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists. [J] . Guo L, Ye Z, Liu J, Bioorganic and Medicinal Chemistry Letters . 2010,第16期

机译：发现有效，选择性和口服生物可利用的3H-螺螺（Isobenzofuran-1,4'-哌啶）的基于Melanocortin亚型-4受体激动剂。
2. Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. [J] . Hong Q, Bakshi RK, Palucki BL, Bioorganic and Medicinal Chemistry Letters . 2011,第8期

机译：发现一种基于哌嗪脲的化合物，该化合物为有效的，选择性的，口服生物利用的黑皮质素亚型4受体部分激动剂。
3. Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist. [J] . He S, Ye Z, Dobbelaar PH, Bioorganic and Medicinal Chemistry Letters . 2010,第7期

机译：发现了一种基于螺茚满的化合物，它是一种有效的，选择性的，口服生物利用的黑皮质素亚型4受体激动剂。
4. Synthesis and in vitro Pharmacological Profile of Potent and Selective Peptidic V1a Receptor Agonists. [C] . Kazinlierz Wisniewski, Robert Galyean, Hiroe Taki American Peptide Symposium . 2009

机译：效力和选择性肽V1A受体激动剂的合成与体外药理学谱。
5. Discovery of INCB9471 a Potent Selective and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity [O] . Chu-Biao Xue, *, Lihua Chen, 2010

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机译：发现A7烟碱乙酰胆碱受体激动剂。（r）-3-（5-氯噻吩-2-基）螺旋-1- azabocyclo 2.2.2辛烷-3，5- 1,3恶唑烷-2-单，为新型，有效，选择性和口服生物可利用的配体

Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists.

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