Abstract：
:We have recently reported the discovery of numerous new compounds that are selective inhibitors of all of the subtypes of the adenosine receptor family via a pharmacophore database searching and screening strategy. During the course of this work we made the unexpected discovery of a potent A(2B) receptor antagonist, 4-methyl-7-methoxyquinazolyl-2-(2'-amino-4'-imidazolinone) (38, CMB 6446), which showed selectivity for this receptor and functioned as an antagonist, with a binding K(i) value of 112 nM. We explored the effects of both substituent- and ring-structural variations on the receptor affinity in this series of derivatives, which were found to be mostly non-selective adenosine receptor ligands with K(i) values in the micromolar range. Since no enhancement of A(2B) receptor affinity of 38 was achieved, the previously reported pharmacophore-based searching strategy yielded the most potent and selective structurally-related hit in the database originally searched.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Webb TR,Lvovskiy D,Kim SA,Ji Xd,Melman N,Linden J,Jacobson KAdoi
10.1016/s0968-0896(02)00323-1subject
Has Abstractpub_date
2003-01-02 00:00:00pages
77-85issue
1eissn
0968-0896issn
1464-3391pii
S0968089602003231journal_volume
11pub_type
杂志文章abstract：:Thirty-three meso-dihydroguaiaretic acid (meso-DGA) derivatives bearing esters, ethers, and amino-ethers were synthesized. All derivatives were tested against twelve drug-resistant clinical isolates of Gram-positive and Gram-negative bacteria, including sensitive (H37Rv) and multidrug-resistant Mycobacterium tuberculo...
journal_title：Bioorganic & medicinal chemistry
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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：2015-05-15 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：2008-05-15 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：2007-01-15 00:00:00
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更新日期：2014-11-01 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：2016-10-15 00:00:00
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pub_type： 杂志文章
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更新日期：2005-05-16 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：2013-11-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
doi：10.1016/j.bmc.2005.02.018
更新日期：2005-04-15 00:00:00
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journal_title：Bioorganic & medicinal chemistry
pub_type： 杂志文章
doi：10.1016/s0968-0896(99)00145-5
更新日期：1999-10-01 00:00:00
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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：2009-03-15 00:00:00
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2019-11-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry
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更新日期：2010-01-15 00:00:00
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更新日期：2006-03-15 00:00:00
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更新日期：2013-09-15 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：2007-11-15 00:00:00
