Carbazates as potent inhibitors of hormone-sensitive lipase
摘要:
The central role of adipose tissue hormone-sensitive lipase in regulating fatty acid metabolism makes it a potential pharmacological target for the prevention of peripheral insulin resistance in obese, prediabetic and diabetic individuals. The synthesis of a new series of carbazates is presented. Modification of the phenolic 4-position in a series of 1,2,3,4-tetrahydroisoquinoline and morpholine derived carbazates, yielded inhibitors of the catalytic activity of this enzyme with nanomolar potency. (C) 2004 Elsevier Ltd. All rights reserved.
Intramolecular Hydroamination of Unbiased and Functionalized Primary Aminoalkenes Catalyzed by a Rhodium Aminophosphine Complex
作者:Lisa D. Julian、John F. Hartwig
DOI:10.1021/ja1052126
日期:2010.10.6
We report a rhodium catalyst that exhibits high reactivity for the hydroamination of primary aminoalkenes that are unbiased toward cyclization and that possess functional groups incompatible with more electrophilic hydroaminationcatalysts. The rhodium catalyst contains an unusual diaminophosphine ligand (L1) that binds to rhodium in a κ(3)-P,O,P mode. The reactions catalyzed by this complex typically
我们报告了一种铑催化剂,它对伯氨基烯烃的加氢胺化表现出高反应性,这些烯烃不偏向环化,并且具有与更多亲电加氢胺化催化剂不相容的官能团。铑催化剂含有一种不寻常的二氨基膦配体 (L1),它以 κ(3)-P,O,P 模式与铑结合。由该配合物催化的反应通常在温和的温度(室温至 70°C)下进行,并且发生在烷基链上缺少取代基的伯氨基烯烃,使系统倾向于环化,伯氨基烯烃含有氯化物、酯、醚、可烯醇化的酮、腈和未保护的醇官能团,以及含有内烯烃的伯氨基烯烃。机理数据表明,这些反应发生的转换限制步骤不同于由 Pd、Pt 和 Ir 的后过渡金属配合物催化的反应。转化限制步骤的这种变化以及由此产生的催化剂的高活性源于 MC 键的质子分解以释放加氢胺化产物与氨基烷基中间体的回复以再生无环前体的有利相对速率。L1 的铑配合物的反应性起源的探针意味着氨基膦基团通过超出空间需求和简单的电子向金属中心的作用导致这些有利的速率。
2-(Dichloroacetyl)-3-substituted-1,2,3,4-tetrahydroisoquinolines as
申请人:Monsanto Company
公开号:US04846880A1
公开(公告)日:1989-07-11
2-(Dichloroacetyl)-3-substituted-1,2,3,4-tetrahydroisoquinoline compounds are antidotes for thiocarbamate, triazine-type and acetamide herbicides. These antidote compounds are especially effective in safening acetamide herbicides used to control grassy and broadleaf weeds in corn.
Methods and compositions for determining the sequence of nucleic acid molecules
申请人:QIAGEN Genomics, Inc.
公开号:US20040115694A1
公开(公告)日:2004-06-17
Methods and compounds, including compositions therefrom, are provided for determining the sequence of nucleic acid molecules. The methods permit the determination of multiple nucleic acid sequences simultaneously. The compounds are used as tags to generate tagged nucleic acid fragments which are complementary to a selected target nucleic acid molecule. Each tag is correlative with a particular nucleotide and, in a preferred embodiment, is detectable by mass spectrometry. Following separation of the tagged fragments by sequential length, the tags are cleaved from the tagged fragments. In a preferred embodiment, the tags are detected by mass spectrometry and the sequence of the nucleic acid molecule is determined therefrom. The individual steps of the methods can be used in automated format, e.g., by the incorporation into systems.
METHODS AND COMPOSITIONS FOR ANALYZING NUCLEIC ACID MOLECULES UTILIZING SIZING TECHNIQUES
申请人:Van Ness Jeffrey
公开号:US20060057566A1
公开(公告)日:2006-03-16
Tags and linkers specifically designed for a wide variety of nucleic acid reactions are disclosed, which are suitable for a wide variety of nucleic acid reactions wherein separation of nucleic acid molecules based upon size is required.
本发明揭示了专门设计用于各种核酸反应的标签和连接剂,适用于需要基于大小分离核酸分子的各种核酸反应。
Methods and compositions for detecting binding of ligand pair using non-fluorescent label
申请人:Rapigene, Inc.
公开号:EP0962464A2
公开(公告)日:1999-12-08
Methods are provided for detecting the binding of a first member to a second member of a ligand pair, comprising the steps of (a) combining a set of first tagged members with a biological sample which may contain one or more second members, under conditions, and for a time sufficient to permit binding of a first member to a second member, wherein said tag is correlative with a particular first member and detectable by non-fluorescent spectrometry, or potentiometry; (b) separating bound first and second members from unbound members; (c) cleaving the tag from the tagged first member; and (d) detecting the tag by non-fluorescent spectrometry, or potentiometry, and therefrom detecting the binding of the first member to the second member.