5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.

Surman MD; Freeman EE; Grabowski JF; Hadden M; Henderson AJ; Jiang G; Jiang XM; Luche M; Khmelnitsky Y; Vickers S; Viggers J; Cheetham S; Guzzo PR

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5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.

机译：作为MCH-1拮抗剂的5-（吡啶基-1-基）吲唑和5-（呋喃基基-5-基）吲唑。

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A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl)indazoles to give 5-(furopyridinon-5-yl)indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy.

机译：合成了一系列具有MCH-1拮抗活性的5-（吡啶-1-基）吲唑。在微型补片钳测定法中，基于这些化合物与hERG钾通道的相互作用，评估了这些化合物的潜在心血管风险。在为期5天的饮食诱导的肥胖小鼠模型中研究了所选化合物，以评估其作为减肥药的潜在用途。 5-（吡啶基-1-基）吲唑的结构修饰以得到5-（呋喃基基-5-基）吲唑，提供了具有增强的药代动力学性质和改善的功效的化合物。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共5页
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Surman MD; Freeman EE; Grabowski JF; Hadden M; Henderson AJ; Jiang G; Jiang XM; Luche M; Khmelnitsky Y; Vickers S; Viggers J; Cheetham S; Guzzo PR;
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1. 5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists. [J] . Surman MD, Freeman EE, Grabowski JF, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：作为MCH-1拮抗剂的5-（吡啶基-1-基）吲唑和5-（呋喃基基-5-基）吲唑。
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3. Efficient synthesis of 5-(bromomethyl)- and 5-(aminomethyl)-1-THP-indazole [J] . Jung-Hui Sun, Christopher A.Teleha, jia-Sheng yan The Journal of Organic Chemistry . 1997,第16期

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5. Advances in the synthesis of indazoles: Regioselective C-7 functionalization by directed ortho metalation and progress towards indazole based azaborine compounds. [D] . Cullen, Fu. 2017

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5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.

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