From Ligand to Complexes. Part 2. Remarks on Human Immunodeficiency Virus type 1 Integrase Inhibition by β-Diketo Acid Metal Complexes
摘要:
Previously, we synthesized a series of beta-diketo acid metal complexes as novel HIV-1 integrase (IN) inhibitors (J. Med. Chem. 2006, 46, 4248-4260). Herein, a further extension of this study is reported. First, detailed docking studies were performed in order to investigate the mode of binding in the active site of the free ligands and of their metal complexes. Second, a series of potentiometric measurements were conducted for two diketo acids chosen as model ligands, with Mn2+ and Ca2+, in order to outline a speciation model. Third, we designed and synthesized a new set of complexes with different stoichiometries and tested them in an in vitro assay specific for IN. Finally, we obtained the first X-ray structure of a metal complex with HIV-1 IN inhibition activity. Analysis of these results supports the hypothesis that the diketo acids could act as complexes and form complexes with the metal ions on the active site of the enzyme.
[EN] METHOD OF PREPARING A RING COMPOUND HAVING TWO ADJACENT CHIRAL CENTERS<br/>[FR] PROCEDE DE PREPARATION D'UN COMPOSE CYCLIQUE CONTENANT DEUX CENTRES CHIRAUX ADJACENTS
申请人:ICOS CORP
公开号:WO2004096764A1
公开(公告)日:2004-11-11
A method of synthesizing a chiral compound having a quarternary carbon atom bearing diastereotopic groups from (a) a nitroolefin and (b) an α-substituted β-dicarbonyl or an equivalent compound having an acidic C-H moiety compound is disclosed. A subsequent intramolecular reaction between one of the substituents comprising the stereogenic carbon atom and one of the diastereotopic groups comprising the quaternary carbon atom creates a new compound having two contiguous stereogenic centers, one of which is quaternary, with control over the relative stereochemistry.
GAS SEPARATION MEMBRANE, GAS SEPARATION MODULE, GAS SEPARATOR, AND GAS SEPARATION METHOD
申请人:FUJIFILM Corporation
公开号:US20180290111A1
公开(公告)日:2018-10-11
A gas separation membrane includes a gas separation layer containing a polyimide compound, in which the polyimide compound has a repeating unit represented by Formula (I),
in Formula (I), R
f1
to R
f6
each independently represent a hydrogen atom or a substituent, a ring Ar
1
and a ring Ar
2
each independently represent an aromatic ring, A represents a single bond or a divalent linking group, and R represents a mother nucleus having a specific structure.
一种气体分离膜包括含有聚酰亚胺化合物的气体分离层,其中聚酰亚胺化合物具有由公式(I)表示的重复单元,
在公式(I)中,R
f1
至R
f6
每个独立地代表一个氢原子或一个取代基,环Ar
1
和环Ar
2
每个独立地代表一个芳香环,A代表一个单键或一个二价连接基团,R代表具有特定结构的母核。
METHOD FOR PRODUCING CARBOXYLIC ACID ANHYDRIDE AND METHOD FOR PRODUCING CARBOXYLIC ACID ESTER
申请人:MITSUBISHI RAYON CO., LTD.
公开号:US20170088502A1
公开(公告)日:2017-03-30
Provided is a production method whereby corresponding carboxylic acid anhydrides and carboxylic acid esters can be obtained at high yield from various carboxylic acids even without a solvent and near room temperature. A method for producing a carboxylic acid anhydride represented by formula (II), the method comprising reacting a compound represented by formula (I) and a carboxylic acid in the presence of a Group II metal compound having an ionic ligand containing an oxygen atom. A method for producing a carboxylic acid ester, the method comprising reacting a carboxylic acid anhydride produced by the aforementioned method and an alcohol. In formula (I), R
1
represents a C
1-20
hydrocarbon group. In formula (II), R
2
represents a C
1-20
hydrocarbon group.
Provided is a production method whereby corresponding carboxylic acid esters can be obtained from a variety of carboxylic acids at a high yield, even under conditions using a simple reaction operation and little catalyst and even if the amount of substrate used is theoretical. A production method for carboxylic acid ester, whereby a prescribed diester dicarbonate, carboxylic acid, and alcohol are reacted in the presence of at least one type of magnesium compound and at least one type of alkali metal compound.
[EN] ACRYLAMIDE-BASED CROSSLINKING MONOMERS, THEIR PREPARATION, AND USES THEREOF<br/>[FR] MONOMÈRES DE RÉTICULATION À BASE D'ACRYLAMIDE, PRÉPARATION ET UTILISATION CORRESPONDANTES
申请人:SALTWORKS TECHNOLOGIES INC
公开号:WO2014059516A1
公开(公告)日:2014-04-24
A process for preparing an acrylamide-based crosslinking monomer comprising reacting in the presence of a catalyst an isocyanate compound containing at least two isocyanate groups with one of acrylic acid or methacrylic acid. These acrylamide-based crosslinking monomers are used in the preparation of coating compositions, adhesive compositions curable by applying thermal or radiation energy, and in the preparation of cation or anion exchange membranes.