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基于吡唑的杂化分子的合成:寻找有效的多药耐药调节剂。

Synthesis of pyrazole-based hybrid molecules: search for potent multidrug resistance modulators.

作者信息

Singh Palwinder, Paul Kamaldeep, Holzer Wolfgang

机构信息

Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, India.

出版信息

Bioorg Med Chem. 2006 Jul 15;14(14):5061-71. doi: 10.1016/j.bmc.2006.02.046. Epub 2006 Mar 22.

Abstract

The hybrid molecules have been designed on the basis of the structural features of pyrazole-based drugs and MDR modulator propafenone. A simple synthetic strategy and solvent-based regioselectivity have been used for the synthesis of newly designed molecules and they are evaluated for their interactions with P-glycoprotein (P-gp). Some of the molecules show considerable interactions with P-gp and compounds 15, 28 and 40 could be the potential candidates for their use as MDR modulators.

摘要

基于吡唑类药物和多药耐药调节剂普罗帕酮的结构特征设计了杂合分子。采用简单的合成策略和基于溶剂的区域选择性来合成新设计的分子,并评估它们与P-糖蛋白(P-gp)的相互作用。其中一些分子与P-gp表现出显著的相互作用,化合物15、28和40可能是用作多药耐药调节剂的潜在候选物。

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