Abstract：
:It has been found that alpha-effects in nucleophilic reactions, unexpectedly large nucleophilicity due to adjacent unpaired electrons, are strongly dependent on the structure of substrate. The nucleophilic cleavages of 4-nitrobenzoate esters and 4-methylbenzoate esters by HOO- have been systematically investigated in detail. When the leaving groups of substrates are sufficiently good (aryl, 2,2,2-trifluoroethyl, and 2,2-dichloroethyl esters), alpha-effect is evident. However, this effect drastically decreases as the leaving group gets poorer, and is only marginal for the cleavages of 2-fluoroethyl and methyl esters. In the nucleophilic cleavages by salicylaldoxime and acetohydroxamic acid, alpha-effect is also notable only for the esters having good leaving groups. These enormous dependences of alpha-effects on the substrate-structure have been interpreted in terms of the difference in the position of transition-state in the reaction coordinate.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Nomura Y,Kubozono T,Hidaka M,Horibe M,Mizushima N,Yamamoto N,Takahashi T,Komiyama Mdoi
10.1016/j.bioorg.2003.09.003subject
Has Abstractpub_date
2004-02-01 00:00:00pages
26-37issue
1eissn
0045-2068issn
1090-2120pii
S0045206803001093journal_volume
32pub_type
杂志文章abstract：:In the present study, 7-subsituted coumarin derivatives were synthesized using various aromatic and heterocyclic amines, and evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk. The most active compounds were evaluated in vitro for 5-lipoxygenase (5-LOX) inhibition. Docking study w...
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更新日期：2007-02-01 00:00:00
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更新日期：2002-02-01 00:00:00
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pub_type： 杂志文章
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更新日期：2017-02-01 00:00:00
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journal_title：Bioorganic chemistry
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更新日期：2005-06-01 00:00:00
abstract：:Five novel 1H-pyrrolo[2,3-b]pyridine or 1H-pyrazolo[3,4-b]pyridine derivatives, with a methylene, sulfur, sulfoxide or cyclopropyl group as a linker, were designed, synthesized and biologically evaluated against c-Met and ALK. The development of these methods of compound synthesis may provide an important reference fo...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
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更新日期：2016-04-01 00:00:00
