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新型复合丁基芳基哌嗪-1-基衍生物的合成与结构评价

Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives.

作者信息

Szulczyk Daniel, Bielenica Anna, Dobrowolski Michał A, Dobrzycki Lukasz, Krawiecka Mariola, Kuran Bożena, Struga Marta

机构信息

Department of Medical Chemistry, Faculty of Medicine, Medical University of Warsaw, Oczki 3 Street, 02-007 Warsaw, Poland.

Faculty of Chemistry, University of Warsaw, Pasteura 1 Street, 02-093 Warsaw, Poland.

出版信息

Med Chem Res. 2014;23(3):1519-1536. doi: 10.1007/s00044-013-0740-z. Epub 2013 Sep 3.

DOI:10.1007/s00044-013-0740-z
PMID:24489455
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3905170/
Abstract

A series of arylpiperazine derivatives of 1,16-diphenyl-19-azahexacyclo-[14.5.1.0.0.0.0]docosa-2,3,5,7,8,9,11,13,14-nonaene-18,20,22-trione and 4,10-diphenyl-1,2,3,5-indeno[1,2-]isoindole-1,3,5-trione was synthesized. The pharmacological profile of compound at the 5-HT receptor was measured by binding assay. The title compounds were tested in cell-based assay against the human immunodeficiency virus type-1. The X-ray crystallographic studies of derivatives , , , , , and were presented.

摘要

合成了一系列1,16 - 二苯基 - 19 - 氮杂十六环 - [14.5.1.0.0.0.0]二十二碳 - 2,3,5,7,8,9,11,13,14 - 九烯 - 18,20,22 - 三酮和4,10 - 二苯基 - 1,2,3,5 - 茚并[1,2 - ]异吲哚 - 1,3,5 - 三酮的芳基哌嗪衍生物。通过结合试验测定了化合物在5 - HT受体上的药理学特征。对标题化合物进行了针对1型人类免疫缺陷病毒的基于细胞的试验。给出了衍生物、、、、、和的X射线晶体学研究结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/7430cf07e8df/44_2013_740_Fig13_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/2863ad44b778/44_2013_740_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/1a9f5e6061a2/44_2013_740_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/7430cf07e8df/44_2013_740_Fig13_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/363fc1216dd3/44_2013_740_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/daa017b5fa61/44_2013_740_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/ccb6c942805f/44_2013_740_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/8bcfd9195881/44_2013_740_Sch3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/fb58c264f539/44_2013_740_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/fa7f285dfcea/44_2013_740_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/103d91332b38/44_2013_740_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/0c16f19c8f44/44_2013_740_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/0f1018e454ac/44_2013_740_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/41c315578e61/44_2013_740_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/08d4a4b48483/44_2013_740_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/60d8e1469576/44_2013_740_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/8883471519f6/44_2013_740_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/2863ad44b778/44_2013_740_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/1a9f5e6061a2/44_2013_740_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b8/3905170/7430cf07e8df/44_2013_740_Fig13_HTML.jpg

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