1,3,5-三取代 4,5-二氢吡唑作为潜在的大麻素 CB(1)受体拮抗剂的合成、SAR 及分子内氢键模式。
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists.
机构信息
Solvay Pharmaceuticals, Research Laboratories, Chemical Design & Synthesis Unit, C. J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1752-7. doi: 10.1016/j.bmcl.2010.01.049. Epub 2010 Jan 20.
PMID:20137935
Abstract
The synthesis, structure-activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6-18 represent a novel class of potent and selective CB(1) receptor antagonists. Based on X-ray diffraction data, the orally active 17 is shown to elicit a different intramolecular H-bonding mode as compared to ibipinabant (3) and SLV330 (4).
摘要
描述了 1,3,5-三取代 4,5-二氢吡唑的合成、构效关系（SAR）研究和分子内氢键模式。目标化合物 6-18 代表了一类新型的强效和选择性 CB(1)受体拮抗剂。根据 X 射线衍射数据，显示出具有口服活性的 17 与 ibipinabant（3）和 SLV330（4）相比，具有不同的分子内氢键模式。
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