CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS
申请人:Bapat Abhijit S.
公开号:US20140364595A1
公开(公告)日:2014-12-11
The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; or (iv) (AFA)
m″
-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
该发明提供了由至少一种抗真菌剂或抗菌剂与至少一种连接剂和/或载体偶联形成的基于共轭的抗真菌或抗菌前药。这些前药的公式为:(i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; 或 (iv) (AFA)
m″
-X,其中:AFA是抗真菌剂或抗菌剂;L是载体;X是连接剂;m范围从1到10;n范围从2到10;m′为1到10;p为1到10;n′为1到10;q为1到10,前提是q'和n不同时为1;m″为1到10。该发明还提供了包含基于共轭的前药的纳米粒子。此外,该发明还提供了以纳米粒子形式的非共轭抗真菌和抗菌剂。
[EN] FORCE-RESPONSIVE POLYMERSOMES AND NANOREACTORS; PROCESSES UTILIZING THE SAME<br/>[FR] POLYMERSOMES ET NANORÉACTEURS SENSIBLES À LA FORCE; PROCÉDÉS LES UTILISANT
申请人:ADOLPHE MERKLE INSTITUTE UNIV OF FRIBOURG
公开号:WO2019034597A1
公开(公告)日:2019-02-21
The mechanically induced melting properties of DNA were employed to achieve force labile membranes is described. Nucleobase pairs were used as mechanophores. Adenine and thymine functionalized complementary amphiphilic block copolymers were self-assembled into polymersomes. The nucleobases formed hydrogen bonds which were disrupted upon force stimulation. The exposure of the disconnected nucleobases to the hydrophobic matrix of the membranes lead to a change of permeability which permitted the exchange of water-soluble molecules throughout the polymer matrix. Moreover, the encapsulation of horseradish peroxidase enabled the reaction of luminol with hydrogen peroxide to yield a luminescence producing species similar to the marine bioluminescence. Moreover, the same nano-reactors were employed to catalyze the formation of a polyacrylamide gel when force was applied. Insights into the change of permeability of supramolecular networks upon force are provided. These systems are useful for drug delivery, as nanoreactors and for the selective release of curing agents for 3D printing, or fragrances.
Radical Dehydroxylative Alkylation of Tertiary Alcohols by Ti Catalysis
作者:Hao Xie、Jiandong Guo、Yu-Quan Wang、Ke Wang、Peng Guo、Pei-Feng Su、Xiaotai Wang、Xing-Zhong Shu
DOI:10.1021/jacs.0c07492
日期:2020.9.30
coupling partners, including allylic carboxylates, aryl and vinyl electrophiles, and primary alkyl chlorides/bromides, making the method complementary to the cross-coupling procedures. The method is highlyselective for the alkylation of tertiary alcohols, leaving secondary/primary alcohols (benzyl alcohols included) and phenols intact. The synthetic utility of the method is highlighted by its 10-gram-scale
醇的脱氧自由基 CC 键形成反应是合成化学中长期存在的挑战,目前的方法依赖于多步骤程序。在此,我们报告了叔醇的直接脱羟基自由基烷基化反应。这一新协议显示了从醇类中生成叔碳自由基的可行性,并为轻松精确地构建全碳四元中心提供了一种方法。该反应在醇和活化烯烃的广泛底物范围内进行。它可以耐受各种亲电偶联伙伴,包括烯丙基羧酸盐、芳基和乙烯基亲电试剂以及伯烷基氯/溴化物,使该方法与交叉偶联程序形成互补。该方法对叔醇的烷基化具有高度选择性,保持仲醇/伯醇(包括苯甲醇)和酚类完好无损。该方法的合成效用因其 10 克规模的反应和复杂分子的后期修饰而突出。实验和 DFT 计算的组合建立了一个合理的机制,暗示通过 Ti 催化的 C-OH 键均裂产生叔碳自由基。
HETEROCYCLIC IONIC LIQUIDS
申请人:NOHMs Technologies, Inc.
公开号:US20170305869A1
公开(公告)日:2017-10-26
An ionic liquid compound includes an azepanium-functionalized cation. An electrochemical cell electrolyte for an electrical energy storage device includes the ionic liquid compound, aprotic organic solvent, alkali metal salt and an additive.
Studies in pyrolysis. Part XXVI. Model systems for the pyrolysis of poly(ethylene fumarate) and allied polyesters
作者:R. L. Forman、H. M. Mackinnon、P. D. Ritchie
DOI:10.1039/j39680002016
日期:——
Pyrolysis of ethyl maleate leads to cis→trans inversion, with concurrent alkyl–oxygen scission (A1; predominating), acyl–oxygen scission (B2), and decarboxylation (C2). For methyl maleate, A1 scission is structurally precluded; there is cis→trans inversion, with concurrent B2 and C2 scission. Ethylene diacrylate and dimethacrylate both undergo a predominating double C2 scission, in competition with