77372-56-6Relevant academic research and scientific papers
Antibiotic Conjugates with an Artificial MECAM-Based Siderophore Are Potent Agents against Gram-Positive and Gram-Negative Bacterial Pathogens
Br?nstrup, Mark,Grunenberg, J?rg,Hotop, Sven-Kevin,Karge, Bianka,Lai, Yi-Hui,Peukert, Carsten,Pinkert, Lukas,Schulze, Lara Marie
, p. 15440 - 15460 (2021/10/25)
The development of novel drugs against Gram-negative bacteria represents an urgent medical need. To overcome their outer cell membrane, we synthesized conjugates of antibiotics and artificial siderophores based on the MECAM core, which are imported by bacterial iron uptake systems. Structures, spin states, and iron binding properties were predicted in silico using density functional theory. The capability of MECAM to function as an effective artificial siderophore in Escherichia coli was proven in microbiological growth recovery and bioanalytical assays. Following a linker optimization focused on transport efficiency, five β-lactam and one daptomycin conjugates were prepared. The most potent conjugate 27 showed growth inhibition of Gram-positive and Gram-negative multidrug-resistant pathogens at nanomolar concentrations. The uptake pathway of MECAMs was deciphered by knockout mutants and highlighted the relevance of FepA, CirA, and Fiu. Resistance against 27 was mediated by a mutation in the gene encoding ExbB, which is involved in siderophore transport.
Chemically Triggered Synthesis, Remodeling, and Degradation of Soft Materials
Anslyn, Eric V.,Bachman, James L.,Chwatko, Malgorzata,Lee, Doo-Hee,Lynd, Nathaniel A.,Reuther, James F.,Sun, Xiaolong
supporting information, p. 3913 - 3922 (2020/03/10)
Polymer topology dictates dynamic and mechanical properties of materials. For most polymers, topology is a static characteristic. In this article, we present a strategy to chemically trigger dynamic topology changes in polymers in response to a specific chemical stimulus. Starting with a dimerized PEG and hydrophobic linear materials, a lightly cross-linked polymer, and a cross-linked hydrogel, transformations into an amphiphilic linear polymer, lightly cross-linked and linear random copolymers, a cross-linked polymer, and three different hydrogel matrices were achieved via two controllable cross-linking reactions: reversible conjugate additions and thiol-disulfide exchange. Significantly, all the polymers, before or after topological changes, can be triggered to degrade into thiol- or amine-terminated small molecules. The controllable transformations of polymeric morphologies and their degradation herald a new generation of smart materials.
Corresponding amine nitrile and method of manufacturing thereof
-
Paragraph 0146; 0151, (2018/05/24)
The present invention relates to a nitrile manufacturing method, which has characteristics of significantly-reduced ammonia source consumption, low environmental pressure, low energy consumption, low production cost, high nitrile purity, high nitrile yield and the like compared with the method in the prior art, wherein nitrile having a complicated structure can be obtained through the method. The present invention further relates to a method for producing a corresponding amine from the nitrile.
Corresponding amine nitrile and method of manufacturing thereof
-
Paragraph 0148, (2018/05/24)
The invention relates to a preparation method of nitrile. Compared with the prior art, the preparation method has the characteristics of obvious reduction of the usage amount of ammonia sources, low environmental pressure, low energy consumption, low production cost, high purity and yields of nitrile products, and the like, and can be used for obtaining nitrile with a more complex structure. The invention also relates to a method for preparing corresponding amine with nitrile.
Shape-Persistent [4+4] Imine Cages with a Truncated Tetrahedral Geometry
Lauer, Jochen C.,Zhang, Wen-Shan,Rominger, Frank,Schr?der, Rasmus R.,Mastalerz, Michael
, p. 1816 - 1820 (2018/01/22)
The synthesis of shape-persistent organic cage compounds is often based on the usage of multiple dynamic covalent bond formation (such as imines) of readily available precursors. By careful choice of the precursors geometry, the geometry and size of the resulting cage can be accurately designed and indeed a number of different geometries and sizes have been realized to date. Despite of this fact, little is known about the precursors conformational rigidity and steric preorganization of reacting functional groups on the outcome of the reaction. Herein, the influence of conformational rigidity in the precursors on the formation of a [4+4] imine cage with truncated tetrahedral geometry is discussed.
Corresponding amine nitrile and method of manufacturing thereof (by machine translation)
-
Paragraph 0149, (2017/10/22)
The invention relates to a method of manufacturing one kind of nitrile, compared with the prior art, has significantly reduced the amount of ammonia, the environmental pressure of the small, low energy consumption, low production cost, nitrile product purity and yield and the like, and can obtain more complex structure of the nitriles. The invention also relates to the corresponding amine by the nitrile manufacture method. (by machine translation)
Rationally designed cooperatively enhanced receptors to magnify host-guest binding in water
Gunasekara, Roshan W.,Zhao, Yan
supporting information, p. 843 - 849 (2015/01/30)
When disengaged interactions within a receptor are turned on by its guest, these intrahost interactions will contribute to the overall binding energy. Although such receptors are common in biology, their synthetic mimics are rare and difficult to design. By engineering conflictory requirements between intrareceptor electrostatic and hydrophobic interactions, we enabled complementary guests to eliminate the "electrostatic frustration" within the host and turn on the intrahost interactions. The result was a binding constant of Ka >105 M-1 from ammonium-carboxylate salt bridges that typically function poorly in water. These cooperatively enhanced receptors displayed excellent selectivity in binding, despite a large degree of conformational flexibility in the structure.
SUBSTITUTED AROMATIC COMPOUND, HYDROGELATION AGENT, HYDROGEL, AND METHOD FOR GELATING AQUEOUS SAMPLE
-
Paragraph 0128; 0129; 0130; 0131, (2014/01/23)
According to the present invention, a substituted aromatic compound represented by the following general formula (I) is provided. In general formula (I), A1, A2, and A3 each independently represent an aryl group substituted by a hydrophilic group.
Connection of metallamacrocycles via dynamic covalent chemistry: A versatile method for the synthesis of molecular cages
Granzhan, Anton,Schouwey, Clement,Riis-Johannessen, Thomas,Scopelliti, Rosario,Severin, Kay
supporting information; experimental part, p. 7106 - 7115 (2011/06/26)
A modular approach for the synthesis of cage structures is described. Reactions of [(arene)RuCl2]2 [arene = p-cymene, 1,3,5-C6H3Me3, 1,3,5-C6H 3(i-Pr)3] with formylsub
Self-assembly of ball-shaped molecular complexes in water
Grawe, Thomas,Schrader, Thomas,Zadmard, Reza,Kraft, Arno
, p. 3755 - 3763 (2007/10/03)
We present a simple and versatile access to spheroidal molecular assemblies with pronounced stability in highly polar solvents. These complexes are composed of doubly and triply charged complementary building blocks based on ammonium or amidinium cations
