Structural regulation and polishing performance of dendritic mesoporous silica (D-mSiO2) supported with samarium-doped cerium oxide composites

Ceria (CeO₂) particles are prevalent polishing abrasive materials. Trivalent lanthanide ions are the popular category of dopants for enriched surface defects and thus improved physicochemical properties, since they are highly compatible with CeO₂ lattices. Herein, a series of dendritic-like mesoporous silica (D-mSiO₂)-supported samarium (Sm)-doped CeO₂ nanocrystals were synthesized via a facile chemical precipitation method. The relation of the structural characteristics and chemical mechanical polishing (CMP) performances were investigated to explore the effect of Sm-doping amounts on the D-mSiO₂/Sm_xCe_1?xO_2?δ (x = 0–1) composite abrasives. The involved low-modulus D-mSiO₂ cores aimed to eliminate surface scratch and damage, resulting from the optimized contact behavior between abrasives and surfaces. The trivalent cerium (Ce³⁺) and oxygen vacancy (V_O) at CeO₂ surfaces were expected to be reactive sites for the material removal process over SiO₂ films. The optimal oxide-CMP performances in terms of removal efficiency and surface quality were achieved by the 40% Sm-doped composite abrasives. It might be attributed to the high Ce³⁺ and V_O concentrations and the enhancement of tribochemical reactivity between CeO₂SiO₂ interfaces. Furthermore, the relationship between the surface chemistry, polishing performance as well as the actual role in oxide-CMP of the D-mSiO₂/Sm_xCe_1?xO_2?δ abrasives were also discussed.     

Adenine-functionalized conjugated polymer as an efficient photocatalyst for hydrogen evolution from water

Conjugated polymers have emerged as a promising class of organic photocatalysts for photocatalytic hydrogen evolution from water splitting due to their adjustable chemical structures and electronic properties. However, developing highly efficient organic polymer photocatalysts with high photocatalytic activity for hydrogen evolution remains a significant challenge. Herein, we present an efficient approach to enhance the photocatalytic performance of linear conjugated polymers by modifying the surface chemistry via introducing a hydrophilic adenine group into the side chain. The adenine unit with five nitrogen atoms could enhance the interaction between the surface of polymer photocatalyst and water molecules through the formation of hydrogen bonding, which improves the hydrophilicity and dispersity of the resulting polymer photocatalyst in the photocatalytic reaction solution. In addition, the strong electron-donating ability of adenine group with plentiful nitrogen atoms could promote the separation of light-induced electrons and holes. As a result, the adenine-functionalized conjugated polymer PF6A-DBTO2 shows a high photocatalytic activity with a hydrogen evolution rate (HER) of 25.21 mmol g^?1 h^?1 under UV-Vis light irradiation, which is much higher than that of its counterpart polymer PF6-DBTO2 without the adenine group (6.53 mmol g^?1 h^?1). More importantly, PF6A-DBTO2 without addition of a Pt co-catalyst also exhibits an impressive HER of 21.93 mmol g^?1 h^?1 under visible light (λ > 420 nm). This work highlights that it is an efficient strategy to improve the photocatalytic activity of conjugated polymer photocatalysts by the modification of surface chemistry.     

Coupling Interrupted Fischer and Multicomponent Joullié-Ugi to Chase Chemical Diversity: from Batch to Sustainable Flow Synthesis of Peptidomimetics

The generation of peptidomimetic substructures for medicinal chemistry purposes requires effective and divergent synthetic methods. We present in this work an efficient flow process that allows quick modulation of reagents for Joullié-Ugi multicomponent reaction, using spiroindolenines as core motifs. This sterically hindered imine equivalent could successfully be diversified using various isocyanides and amino acids in generally good space-time yields. A telescoped flow process combining interrupted Fischer reaction for spiroindolenine synthesis and subsequent Joullié-Ugi-type modification resulted in product formation in very good overall yield in less than 2 hours compared to 48 hours required in batch mode. The developed protocol can be seen as a general tool for rapid and facile generation of peptidomimetic compounds. We also showcase preliminary biological assessments for the prepared compounds.     

The Young Scientists Network: How the European Federation for Medicinal Chemistry (EFMC) Became Young Again

The European Federation for Medicinal Chemistry (EFMC) created the Young Scientists Network (YSN) to support early-career medicinal chemists and chemical biologists. By doing this, it addressed the rapid changes taking place in the scientific community and in our society, such as the rise of social media, the evolution of the gender balance in the scientific population, and educational needs. Creating the YSN was also a way to ensure that the next generation of scientists would contribute to shaping EFMC's strategy, while recognizing and addressing their needs. The YSN was set up as a very dynamic concept, and has now developed to the point where its impact is evident. The activities it promotes complement EFMC's community support and scientific opportunities, rejuvenating the Federation and preparing it for the future. It also provides opportunities for many brilliant young scientists, who do not hesitate to invest time and energy in supporting our community and shaping their own future.     

Advanced Functional Materials Constructed from Pillar[n]arenes

Pillar[n]arenes are new generation of supramolecular macrocyclic host, which exhibit excellent host−guest recognition properties. In the last decade, functional materials constructed from pillar[n]arenes have been attracted more and more attention and displayed outstanding characteristics, such as stimuli-responsiveness, self-healing and adaptability. In this mini-review, we provide a survey of the pillar[n]arene-based literatures covering light-harvesting systems, functional hydrogels, and solid materials. It is anticipated that more and more pillar[n]arenes-based advanced materials with multi-functional properties will appear in the near future.     

Broad-Spectrum Flavivirus Inhibitors: a Medicinal Chemistry Point of View

Infections by flaviviruses, such as Dengue, West Nile, Yellow Fever and Zika viruses, represent a growing risk for global health. There are vaccines only for few flaviviruses while no effective treatments are available. Flaviviruses share epidemiological, structural, and ecologic features and often different viruses can co-infect the same host. Therefore, the identification of broad-spectrum inhibitors is highly desirable either for known flaviviruses or for viruses that likely will emerge in the future. Strategies targeting both virus and host factors have been pursued to identify broad-spectrum antiflaviviral agents. In this review, we describe the most promising and best characterized targets and their relative broad-spectrum inhibitors, identified by drug repurposing/libraries screenings and by focused medicinal chemistry campaigns. Finally, we discuss about future strategies to identify new broad-spectrum antiflavivirus agents.     

Activity of Riminophenazines against Mycobacterium tuberculosis: A Review of Studies that Might be Contenders for Use as Antituberculosis Agents

Tuberculosis is one of the leading cause of death in the world, mainly due to the increasing number of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) strains. Factors such as the HIV pandemic contribute further. Also, the ineffectiveness of the chemotherapy in current use increases the mortality rate. Therefore, new and repurposed antituberculosis drugs are urgently needed for the treatment of MDR-TB, and riminophenazines are among those drugs that are being reinvestigated for their potential in the treatment of TB. This review delivers a brief historical account of riminophenazines, their general synthesis, mechanisms of action, and their physicochemical properties. The discussion is limited to those studies that investigated the activity of these compounds as antituberculosis agents. Given their unique properties, this review will be of great significance in giving direction towards the design and development of new riminophenazine analogues.     

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Pharmacophore searches that include anchors, fragments contributing above average to receptor binding, combined with one-step syntheses are a powerful approach for the fast discovery of novel bioactive molecules. Here, we are presenting a pipeline for the rapid and efficient discovery of aspartyl protease inhibitors. First, we hypothesized that hydrazine could be a multi-valent warhead to interact with the active site Asp carboxylic acids. We incorporated the hydrazine anchor in a multicomponent reaction and created a large virtual library of hydrazine derivatives synthetically accessible in one-step. Next, we performed anchor-based pharmacophore screening of the libraries and resynthesized top-ranked compounds. The inhibitory potency of the molecules was finally assessed by an enzyme activity assay and the binding mode confirmed by several soaked crystal structures supporting the validity of the hypothesis and approach. The herein reported pipeline of tools will be of general value for the rapid generation of receptor binders beyond Asp proteases.