Multicomponent chemistry in the synthesis of carbonic anhydrase inhibitors.

Carbonic anhydrase inhibitors (CAIs) are of growing interest since various isoforms of the enzyme are identified as promising drug targets for treatment of disease. The principal drawback of the clinically used CAIs is the lack of isoform selectivity, which may lead to observable side effects. Studies aiming at the design of isoform-selective CAIs entail generation and biological testing of arrays of compounds, which is a resource- and time-consuming process. Employment of multicomponent reactions is an efficient synthetic strategy in terms of gaining convenient and speedy access to a range of scaffolds with a high degree of molecular diversity. However, this powerful tool appears to be underutilized for the discovery of novel CAIs. A number of studies employing multicomponent reactions in CAI synthesis have been reported in literature. Some of these reports provide inspiring examples of successful use of multicomponent chemistry to construct novel potent and often isoform-selective inhibitors. On critical reading of several publications, however, it becomes apparent that for some chemical series designed as CAIs, the desired inhibitory properties are only assumed and never tested for. In these cases, the biological profile is reported based on the results of phenotypical cellular assays, with no correlation with the intended on-target activity. Present review aims at critically assessing the current literature on the multicomponent chemistry in the CAI design

Sustainable Generation of Ni(OH)2 Nanoparticles for the Green Synthesis of 5-Substituted 1 H-Tetrazoles:A Competent Turn on Fluorescence Sensing of H2O2

A mutually correlated green protocol has been devised that originates from a sustainable production of β-Ni(OH)2 nanoparticles which is used for an efficient catalytic synthesis of versatile substituted tetrazoles, under mild reaction conditions in water via a simple, one-pot, eco-friendly method. The synthesis is followed by derivatization into a highly fluorescence active compound 9-(4-(5-(quinolin-2-yl)-1H-tetrazol-1-yl)phenyl)-9H-carbazole that can be used at tracer concentrations (0.1 μM) to detect as well as quantify hydrogen peroxide down to 2 μM concentration. The nanocatalyst was synthesized by a simple, proficient, and cost-effective methodology and characterized thoroughly by UV-vis absorption and Fourier transform infrared spectra, N2 adsorption/desorption, high resolution transmission electron microscopy, powder X-ray diffraction pattern, field emission scanning electron microscopy, and thermogravimetric analysis. Broad substrate scope, easy handling, higher efficiency, low cost, and reusability of the catalyst are some of the important features of this heterogeneous catalytic system. The strong analytical performance of the resultant derivative in low-level quantification of potentially hazardous hydrogen peroxide is the key success of the overall green synthesis procedure reported here

A comprehensive and critical review on recent progress in anode catalyst for methanol oxidation reaction

The synthesis of anode electrocatalyst with high activity and durability for methanol oxidation reaction has been one of the main focuses of researchers in recent years. Several works are reviewed in this paper to summarize and compare the performance of electrocatalysts comprising of noble and non-noble metals. The effect of manipulating catalysts by introducing nanostructured morphology, metal alloys, support materials, acidic or basic electrolyte, and synthesis methods are also examined. The paper finally concludes with details of challenges that are generally faced in making direct methanol fuel cell (DMFC) a reliable source of energy for future prospects, and the approach to be taken to reduce the complexity in synthesizing new generations of anode electrocatalysts.This publication was made possible by NPRP grant (NPRP8-145-2-066) from the Qatar National Research Fund (a member of Qatar foundation). The statements made herein are solely the responsibility of the author(s). The author(s) would also like to acknowledge the support from Qatar University internal grant QUCG-CENG-19/20-7. Open Access funding provided by the Qatar National Library.Scopu

Synthesis of novel acridine-sulfonamide hybrid compounds as acetylcholinesterase inhibitor for the treatment of alzheimer’s disease

In this study we report that amino acridine intermediates 7 and 8 were obtained from the reduction of nitro acridine derivatives 5 and 6 that were synthesized via the condensation of dimedone, p-nitrobenzaldehyde with various amine derivatives, respectively. Then acridine sulfonamide hybrid compounds (9–18) were synthesized by the reaction of amino acridine 7, 8 with sulfonyl chlorides. The new hybrid compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, and HRMS analyzes. The evaluation of in vitro anticholinesterase action of the synthesized compounds against AChE showed that some of them are potent inhibitors. Among them, compound 17 showed the most potent activity against AChE with an IC50 of 0.14 µM. © 2017, Springer Science+Business Media, LLC