Abstract：
:Three series of new N-substituted 1,2,3,4-tetrahydroisoquinolines with 2-, 3-, and 4-membered alkyl chains (a, b, and c, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A receptor affinities and functional properties was discussed. It was found that the volume of the terminal amide substituent was a crucial parameter which determined 5-HT1A receptor affinities of the tested compounds, while the in vivo activity seemed to depend on both the R-volume and the length of a hydrocarbon chain. It was demonstrated that the most active ligands behaved like agonists or partial agonists at postsynaptic 5-HT1A receptors.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Mokrosz MJ,Bojarski AJ,Duszyńska B,Tatarczyńska E,Kłodzińska A,Dereń-Wesołek A,Charakchieva-Minol S,Chojnacka-Wójcik Edoi
10.1016/s0968-0896(98)00238-7subject
Has Abstractpub_date
1999-02-01 00:00:00pages
287-95issue
2eissn
0968-0896issn
1464-3391pii
S0968-0896(98)00238-7journal_volume
7pub_type
杂志文章abstract：:omega-(1H-Imidazol-4-yl)alkane-1-sulfonamides were prepared and found to be potent histamine H(3) receptor antagonists. High receptor affinity and a low difference in the data between the bioassays were achieved with 5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide (16). Good in vitro profiles were also...
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2000-03-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2007-01-15 00:00:00
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更新日期：2016-02-01 00:00:00
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更新日期：2009-02-15 00:00:00
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更新日期：2017-02-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2012-01-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2008-01-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
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journal_title：Bioorganic & medicinal chemistry
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journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
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更新日期：2009-02-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
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更新日期：2013-09-01 00:00:00
abstract：:This article has been withdrawn at the request of the author(s) and/or editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy. ...
journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
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更新日期：2006-02-21 00:00:00
abstract：:Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC(50) of 16 compounds which have displayed MIC of 0.25 microg/mL were also recorded. One of the compounds (...
journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
doi：10.1016/j.bmc.2008.11.005
更新日期：2009-01-01 00:00:00
