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新型含（2-喹啉基甲氧基）苯基化合物系列作为高亲和力白三烯D4受体拮抗剂的研发。4. 色酮部分的添加增强了白三烯D4受体结合亲和力。

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.

作者信息

Huang F C, Galemmo R A, Poli G B, Learn K S, Morrissette M M, Johnson W H, Dankulich W P, Campbell H F, Carnathan G W, VanInwegen R G

机构信息

Rhone-Poulenc Rorer Central Research, King of Prussia, Pennsylvania 19406.

出版信息

J Med Chem. 1991 May;34(5):1704-7. doi: 10.1021/jm00109a025.

DOI:10.1021/jm00109a025
PMID:1851845
Abstract

The combination of the benzopyran-4-one ring, a moiety found in the prototype leukotriene antagonist, FPL 55,712, with the (2-quinolinylmethoxy)phenyl group led to a significant increase in leukotriene receptor binding affinity. This modification resulted in a 10,000-fold improvement in binding affinity compared to FPL 55,712. Compound 7 (RG 12553), with a Ki value of 0.1 nM, has higher affinity than the natural agonist LTD4 and is one of the most potent LTD4 antagonists reported. The structure-activity relationships of this series of potent leukotriene antagonists are discussed.

摘要

苯并吡喃-4-酮环（原型白三烯拮抗剂FPL 55,712中的一个部分）与(2-喹啉基甲氧基)苯基的结合，使白三烯受体结合亲和力显著提高。与FPL 55,712相比，这种修饰使结合亲和力提高了10000倍。化合物7（RG 12553）的Ki值为0.1 nM，其亲和力高于天然激动剂LTD4，是报道的最有效的LTD4拮抗剂之一。讨论了这一系列强效白三烯拮抗剂的构效关系。

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Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.新型含（2-喹啉基甲氧基）苯基化合物系列作为高亲和力白三烯D4受体拮抗剂的研发。4. 色酮部分的添加增强了白三烯D4受体结合亲和力。
J Med Chem. 1991 May;34(5):1704-7. doi: 10.1021/jm00109a025.
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Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.新型含(2-喹啉基甲氧基)苯基化合物作为高亲和力白三烯D4受体拮抗剂的研发。2. 额外苯环对受体亲和力的影响。
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The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.一系列新型含（喹啉-2-基甲氧基）苯基化合物作为高亲和力白三烯受体拮抗剂的研发。3. 酸性侧链的结构变化以获得效力增强的拮抗剂。
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Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.新型含（2-喹啉基甲氧基）苯基化合物系列作为高亲和力白三烯受体拮抗剂的研发。1. 初步构效关系。
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