Weinreb amide based building blocks for convenient access to various synthetic targets

1749-1756N-Methoxy-N-methylamide, popularly known as the Weinreb amide (WA), has served as an excellent acylating agent for organolithium and/or organomagnesium reagents and a robust equivalent for an aldehyde group. The stability of the WA functionality, its ease of preparation, the scalability of its reactions and its predictable reactivity are the key features responsible for its prominent use in several synthetic endeavors by the chemists world-wide. The development of WA-based building blocks and synthetic equivalents for interesting synthons has been a long drawn pursuit initiated in nineties and through this mini-review accomplishments in this direction, with particular emphasis on the building blocks, developed recently in the last three years are summarized

Fouling and Performance Investigation of Membrane Distillation at Elevated Recoveries for Seawater Desalination and Wastewater Reclamation

This study reports on the impact of elevated recovery (i.e., 80%, 85%, and 90%) on the fouling and performance of air gap membrane distillation (AGMD) with real seawater and landfill leachate wastewater samples using polytetrafluoroethylene (PTFE) polymer membranes. Increasing the feed temperature from 55 °C to 65 °C improved the water flux of seawater and wastewater and shortened the operating time by 42.8% for all recoveries. The average water flux in the 80%, 85%, and 90% recovery experiments at the 65 °C feed temperature was 32%, 37.32%, and 36.7% higher than the case of 55 °C for the same recoveries. The water flux decline was more severe at a higher temperature and recovery. The highest flux decline was observed with a 90% recovery at 65 °C feed temperature, followed by an 85% recovery at 65 °C. Close examination of the foulants layer revealed that seawater formed a cake fouling layer made predominantly of metal oxides. In contrast, the landfill leachate fouling was a combination of pore blocking and cake formation, consisting mainly of carbonous and nitrogenous compounds. Physical cleaning with deionized (DI) water at 55 °C and 65 °C and chemical cleaning with hydrogen peroxide (H2O2) were investigated for their efficiency in removing membrane foulants. Analytical results revealed that seawater fouling caused membrane pore blockage while wastewater fouling formed a porous layer on the membrane surface. The results showed that membrane cleaning with hydrogen peroxide restored >97% of the water flux. Interestingly, the fouling factor in seawater tests was 10%, while it was 16% for the wastewater tests

Interface engineered Ag-r-GO-CuFe\u2082O\u2084-Fe\u2083O\u2081 heterojunction an efficient photocatalyst for water treatment and toxicity study in Trifolium plants

Abstract: Herein, we report the Ag-r-GO-CuFe 2 O 4-Fe 3 O 4 nanocomposite (Ag-r-GO-CFO-FO NCs) for effective photocatalytic activity against organic pollutants. Herein the O-S scheme mechanism is achieved by the formation of Ohmic (O) and Schottky (S) junctions. The two interfacial charge carriers for accelerated phono formation and mass transfer and thus increase in the light-harvesting with electron traps for the gerenation of reactive oxygen species (ROS). The photocatalytic activity of the constructed Ag-r-GO-CFO-FO NCs was tested against organic dyes (red RB, orange 2R and black B) and the degradation efficiency was calculated to be 99.8, 99.3 and 99.8% respectively. The radical quenching shows the formation of center dot OH and O 2 center dot- which plays major role in the mineralization of organic pollutants. Total organic carbon (TOC) after the degradation of red RB, orange 2R and black B by Ag-r-GO-CFO-FO NCs was 2.1%, 1.6% and 1.9% respectively, which shows the complete mineralization of the pollutants. In addition, the real-time application of the photocatalytic efficiency of NCs was performed against the effluent collected from dying industrial (which is a combination of red RB, orange 2R and black B) and the degradation efficiency was 98.2%. Toxicity of the NCs was performed against maize plants, the results show that the NCs are non-toxicity towards plants and can be used for real-time application. The efforts provide evidence of the combination of two interfacial charge carriers (O-S scheme) to boost the catalytic activity of the catalyst for water treatment

The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis

Currently, there are no effective therapies for patients with triple-negative breast cancer (TNBC), an aggressive and highly metastatic disease. Activation of eukaryotic initiation factor 4E (eIF4E) by mitogen-activated protein kinase (MAPK)-interacting kinases 1 and 2 (Mnk1/2) play a critical role in the development, progression and metastasis of TNBC. Herein, we undertook a comprehensive study to evaluate the activity of a first-in-class Mnk1/2 protein degraders, racemic VNLG-152R and its two enantiomers (VNLG-152E1 and VNLG-152E2) in in vitro and in vivo models of TNBC. These studies enabled us to identify racemic VNLG-152R as the most efficacious Mnk1/2 degrader, superior to its pure enantiomers. By targeting Mnk1/2 protein degradation (activity), VNLG-152R potently inhibited both Mnk-eIF4E and mTORC1 signaling pathways and strongly regulated downstream factors involved in cell cycle regulation, apoptosis, pro-inflammatory cytokines/chemokines secretion, epithelial-mesenchymal transition (EMT) and metastasis. Most importantly, orally bioavailable VNLG-152R exhibited remarkable antitumor (91 to 100% growth inhibition) and antimetastatic (~80% inhibition) activities against cell line and patient-derived TNBC xenograft models, with no apparent host toxicity. Collectively, these studies demonstrate that targeting Mnk-eIF4E/mTORC1 signaling with a potent Mnk1/2 degrader, VNLG-152R, is a novel therapeutic strategy that can be developed as monotherapy for the effective treatment of patients with primary/metastatic TNBC