Abstract:
:Starting from substituted 9-chloroacridines, a series of quinacrine and spacered dimeric acridine compounds was prepared. Their ability to interrupt the protein association of prion- and Alzheimer-specific proteins and Ab peptides was explored using a fast screening system based on FACS analysis. The bis-acridines displayed a higher activity than the corresponding monomers. Among these derivatives, best results were obtained with the 2,4-dimethoxy-6-nitro compound 7h for Abeta-peptides and the 2-methoxy-6-nitro compound 7f for PrP.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Csuk R,Barthel A,Raschke C,Kluge R,Ströhl D,Trieschmann L,Böhm Gdoi
10.1002/ardp.200900065subject
Has Abstractpub_date
2009-12-01 00:00:00pages
699-709issue
12eissn
0365-6233issn
1521-4184journal_volume
342pub_type
杂志文章abstract::A series of 5-alkyl-5-phenylbarbituric acid analogues were shown to be potent hypolipidemic agents in rats and mice at 20 mg/kg/day. This dose is lower than that required for hypolipidemic activity for clofibrate and nicotinic acid derivatives in rodents and man. These new derivatives reduced both serum cholesterol an...
journal_title:Archiv der Pharmazie
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doi:10.1002/ardp.19903230905
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abstract::Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested pos...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19953280712
更新日期:1995-07-01 00:00:00
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
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更新日期:2020-06-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.2503241201
更新日期:1991-12-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19953280903
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/1521-4184(200208)335:6<277::AID-ARDP277>3.
更新日期:2002-06-01 00:00:00
abstract::Inhibition of 5-lipoxygenase by anthralin (1) and 41 derivatives is determined: the acids 38 and 39, the lactones 40-42 and 9-anthrone (8) are the most potent inhibitors, the lactone 41 reaching the efficacy of nordihydroguaiaretic acid (NDGA). The results were correlated with the hydrophilic/lipophilic balance of the...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.2503241104
更新日期:1991-11-01 00:00:00
abstract::Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2 ] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxic...
journal_title:Archiv der Pharmazie
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更新日期:2014-05-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:2016-02-01 00:00:00
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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abstract::In the present study, a novel series of polyfunctionalized imidazopyrimidines 6a-u and 9a-d were efficiently constructed by a domino reaction between 2-imino-6-substituted-2,3-dihydropyrimidin-4(1H)-ones 4a-d or 8a-c and 2-bromoacetophenones 5a-i under mild basic conditions. The synthesized series were screened for th...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:2013-01-01 00:00:00
abstract::New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic a...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:1999-06-01 00:00:00
abstract::This paper describes the use of the multivariate image analysis-quantitative structure-activity relationship (MIA-QSAR) methodology, which is a method capable of relating chemical structures with their biological activities. This in silico method has been shown to be extremely reliable and provides excellent results, ...
journal_title:Archiv der Pharmazie
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更新日期:2012-09-01 00:00:00