Novel delta dicarbonyl compounds and methods for using the same
申请人:——
公开号:US20020137775A1
公开(公告)日:2002-09-26
Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH
2
group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.
The present invention relates to norbormide analogues having rodenticidal activity; rodenticidal compositions comprising the analogues; uses of the analogues as rodenticides; uses of the analogues in the manufacture of rodenticidal compositions; and methods for controlling rodents using the compositions.
Acyloxymethyl and alkoxycarbonyloxymethyl prodrugs of a fosmidomycin surrogate as antimalarial and antibacterial agents
作者:Charlotte Courtens、Frits van Charante、Thibaut Quennesson、Martijn Risseeuw、Paul Cos、Guy Caljon、Tom Coenye、Serge Van Calenbergh
DOI:10.1016/j.ejmech.2022.114924
日期:2023.1
inability to penetrate the bacterial cell wall. Temporarily masking the phosphonate moiety as a prodrug has the potential to solve both issues. We report on the expansion of the acyloxymethyl and alkoxycarbonyloxymethyl phosphonate ester prodrug series of a fosmidomycin surrogate. Prodrug promoieties were designed based on electronic, lipophilic and siderophoric properties. This investigation led to the discovery
Fosmidomycin 是一种天然抗生素,具有有效的 IspC(DXR,1-脱氧-d-木酮糖-5-磷酸还原异构酶)抑制活性。这种酶催化非甲羟戊酸类异戊二烯生物合成途径的第一个关键步骤,这在大多数细菌(包括鲍曼不动杆菌和结核分枝杆菌)和顶复门寄生虫(包括疟原虫寄生虫)中必不可少。主要由于其高极性,磷米霉素表现出次优的药代动力学特性。此外,fosmidomycin 对鲍曼不动杆菌和结核分枝杆菌无活性由于其无法穿透细菌细胞壁。暂时将膦酸酯部分作为前药进行掩蔽有可能解决这两个问题。我们报告了磷胺霉素替代物的酰氧基甲基和烷氧基羰基氧基甲基膦酸酯前药系列的扩展。前药前体是根据电子、亲脂性和铁载体特性设计的。该研究导致发现了分别具有两位数纳摩尔和亚微摩尔 IC 50值的衍生物,用于对抗恶性疟原虫和鲍曼不动杆菌。
[EN] CATALYSED ALTERNATING COPOLYMERISATION AND PRODUCT
申请人:——
公开号:WO1981001289A1
公开(公告)日:1981-05-14
(EN) A Process for the preparation of a copolymer comprising sequences of alternating monomer residues, which process comprises reacting at least one donor monomer with at least one acceptor monomer in the presence of: 1) a transition metal complex comprising at least one (Alpha)-acid ligand; 2) an organic compound, which may be a polymer, comprising at least one carbon-halogen bond, an acetylenic bond or an ethylenic bond conjugated with one or more electron attracting (-R) groups; and 3) a Lewis acid. (FR) Procede de preparation d'un copolymere comprenant des sequences de restes monomeres alternes, ce procede se basant sur la reaction entre au moins un monomere donneur et un monomere accepteur en presence de: (i) un complexe de metal de transition comprenant au moins un groupe de coordination (Alpha)-acide; (ii) un compose organique, qui peut etre un polymere, comprenant au moins une liaison carbone-halogene, une liaison acetylenique ou une liaison ethylenique conjuguee avec un ou plusieurs groupes d'attraction d'electrons (-R); et (iii) un acide de Lewis.