含修饰的4-哌啶基-2-苯基-1-(苯磺酰氨基)丁烷的CCR5拮抗剂的合成与评价
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
作者信息
Shah Shrenik K, Chen Natalie, Guthikonda Ravindra N, Mills Sander G, Malkowitz Lorraine, Springer Martin S, Gould Sandra L, Demartino Julie A, Carella Anthony, Carver Gwen, Holmes Karen, Schleif William A, Danzeisen Renee, Hazuda Daria, Kessler Joseph, Lineberger Janet, Miller Michael, Emini Emilio A, MacCoss Malcolm
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 15;15(4):977-82. doi: 10.1016/j.bmcl.2004.12.044.
Synthesis of analogs containing more rigid bicyclic piperidine replacements for the 4-benzyloxycarbonyl-(ethyl)amino-piperidine moiety of the CCR5 antagonist structure, 1, is described. Although similar binding affinity to the lead was achieved with some analogs they were overall less potent anti-HIV agents suggesting that other features besides CCR5 binding are required for good anti-viral activity.
描述了用于CCR5拮抗剂结构1的4-苄氧羰基-（乙基）氨基哌啶部分的含有更刚性双环哌啶取代基的类似物的合成。尽管一些类似物实现了与先导物相似的结合亲和力，但它们总体上是效力较低的抗HIV药物，这表明除了CCR5结合外，良好的抗病毒活性还需要其他特征。
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