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A bright future for small molecules: Drugs based on molecules made by chemists are far from old-fashioned. Although biopharmaceuticals developed during the last two decades may have caught the public's imagination, traditional drugs remain a strong force in the pharmaceutical industry. Effective, inexpensive small-molecule drugs are crucial in fighting diseases and maintaining cost-effective health care.  相似文献   

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Knowledge about the structural and biophysical properties of proteins when they are free in solution and/or in complexes with other molecules is essential for understanding the biological processes that proteins regulate. Such knowledge is also important to drug discovery efforts, particularly those focused on the development of therapeutic agents with protein targets. In the last decade a variety of different covalent labeling techniques have been used in combination with mass spectrometry to probe the solution-phase structures and biophysical properties of proteins and protein—ligand complexes. Highlighted here are five different mass spectrometry—based covalent labeling strategies including: continuous hydrogen/deuterium (H/D) exchange labeling, hydroxyl radical-mediated footprinting, SUPREX (stability of unpurified proteins from rates of H/D exchange), PLIMSTEX (protein-ligand interaction by mass spectrometry, titration, and H/D exchange), and SPROX (stability of proteins from rates of oxidation). The basic experimental protocols used in each of the above-cited methods are summarized along with the kind of biophysical information they generate. Also discussed are the relative strengths and weaknesses of the different methods for probing the wide range of conformational states that proteins and protein-ligand complexes can adopt when they are in solution.  相似文献   

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The organocalcium chemistry developed vastly during the last decade. The preparation of the organocalcium compounds via direct synthesis (insertion of Ca into a C‐X bond of phenyl halides, Grignard reaction) affords skilful procedures due to the inertia of the calcium metal and the extreme reactivity of the organocalcium derivatives. Further suitable preparative methods include metathesis reactions of CaX2 with KR or LiR, metallation reactions of H‐acidic substrates, metal‐halogen exchange reactions, and transmetallation of heavy main group atoms in their compounds with calcium metal. Possibilities to stabilize organocalcium compounds include steric shielding by bulky ligands at the periphery and electronic reduction of the nucleophilicity of the calcium‐bound carbanions. Selected applications in catalysis such as hydrophosphination are also mentioned. Very recent developments and challenges in the preparation of alkaline earth metal(I) compounds are presented as well. Concepts to overcome the rather large atomization energies of the metals are discussed.  相似文献   

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In assemblies of identical molecules or chromophores, electronic excitations can be described as excitons, bound electron-hole pairs that can move from site to site as a pair in a coherent manner. The understanding of excitons is crucial when trying to engineer favorable photophysical properties through structuring organic molecular matter. In recent decades, limitations of the concept of an exciton have become clear. The exciton can hybridize with phonon and photons. To clarify these issues, the exciton is discussed within the broader context of the gauge properties of the electromagnetic force.  相似文献   

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Benserazide (D, L-serine-2-[2,3,4-(trihydroxyphenyl)methyl]hydrazide) is one of aroma- tic L-amino acid decarboxylase inhibitors, and used with levodopa for treatment of Parkinson’s disease1. Hence, determination of benserazide is an indispensable program. Recently, chromatography2, spectrophotometry3,4 and capillary electrophoresis5 have been used for the determination of benserazide. However, these methods are low sensitive and inconvenient. In order to search new method for detecting ben…  相似文献   

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Good research data management (RDM) requires a constant endeavour of the researchers but – first and foremost – user-friendly infrastructure and well accepted standards need to be developed for the researchers. The national research data infrastructure initiative for chemistry in Germany NFDI4Chem sets out to embrace the challenge of creating a general research data management portal and hereby connecting already existing infrastructure as well as to foster the cultural change in chemistry towards digitalization by developing general minimum information standards for all methods used and teaching RDM principles to the community. In order to serve the needs of the chemical community at its best, NFDI4Chem accomplishes regular community surveys. The first survey has been performed in 2019 and the results were condensed into the NFDI4Chem proposal. This article summarizes the design of the study and its results. With regard to the project development, this first national survey serves as zero-point of all upcoming efforts in research data management.  相似文献   

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The propellent drive and development opportunities for future catalytic technologies in petrochemical industry in the 21st century are reviewed in this paper. It focuses on the following five aspects: (1) The environmentally-friendly catalytic technologies, such as new technologies for the production of organic chemicals changing the raw material and synthetic process, the chemicals production replacing phosgene and hydrogen cyanide toxicant, and the conversion and utilization of organic waste…  相似文献   

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The element nitrogen is essential to life. Considerable attention is thus paid to the development of synthetic methods for its introduction into molecules. Nitrenes, long regarded as highly reactive but poorly selective species, have recently emerged as useful tools for the formation of C-N bonds. Practical metal-catalyzed protocols are now available for the preparation of amines through either the aziridination of alkenes or the C-H amination of alkanes. Recent results highlighted in this Minireview suggest that synthetic nitrene chemistry is maturing with a wider scope not limited to these two reactions.  相似文献   

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The discovery of the ozone hole over Antarctica in 1985 was a surprise for science. For a few years the reasons of the ozone hole was speculated about. Soon it was obvious that predominant meteorological conditions led to a specific situation developing in this part of the atmosphere: Very low temperatures initiate chemical processes that at the end cause extreme ozone depletion at altitudes of between about 15 and 30 km. So‐called polar stratospheric clouds play a key role. Such clouds develop at temperatures below about 195 K. Heterogeneous chemical reactions on cloud particles initiate the destruction of ozone molecules. The future evolution of the ozone layer will not only depend on the further development of concentrations of ozone‐depleting substances, but also significantly on climate change.  相似文献   

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JackHolbrook 《化学教育》2002,23(12):11-14,33
While chemistry is popular for children of primary school age,its popularity drops dramatically in secondary schools,A potential solution to address this is to recognise the need for greater relevance-relevance to the curriculum,to the needs of society and,in the eyes of the students.The paper tries to puts forward a rethink of the philosophy for school chemistry education,based on the underlying belief that chemistry education is an integral part of education.The target is labelled scientific and technological literacy for all (STL),STL rejects the notion that chemistry is taught solely to acquire tha abilities to be a scientist and supports the vision of a single curriculum goal,applicable to all students.Besides being a philosophy,STL is also a teaching approach.This approach is to initiate the teaching of chemistry topics,starting from a carefully chosen society perspective and to introduce the conceptual learning on a need-to-know basis.A limitatioin is the professional development of teachers,Suggestion for overcoming this involve workshop on materials development.Aconcern is expressed in cases where teachers make use of ready-made teaching materials(a common practice),without first gaining an understanding and an appreciation of the intended philosophy related to these materials.  相似文献   

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Cristina Viano 《Ambix》2015,62(3):203-214
In On Generation and Corruption 1.10, Aristotle introduces the new idea of “chemical mixture” (mixis) to explain the constitution of those homogeneous substances from which all things in the sublunary world are comprised. In a mixture, the ingredients interact with one another to give rise to a new substance, qualitatively different, yet preserving the original ingredients in potentia, so that they can be separated again. In Book IV of the Meteorologica, Aristotle further suggests that bodies may be “diagnosed” according to certain passive properties, such as the fusibility of metals. While his theory of mixture has often led historians of science to identify Aristotle as one of the precursors of chemical science, his ideas have also been criticised as archaic, and implicated in a qualitative conception of the cosmos that delayed progress towards quantifying natural phenomena. In this paper, I take up the defence of Aristotle's theory by showing that his concept of mixture is not an obstacle to the development of natural science and chemistry, but, on the contrary, opens the way by offering an advanced model of qualitative analysis which does not exclude the possibility of quantitative development.  相似文献   

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