468087-07-2

Upstream product

• 17754-90-4 4-(Diethylamino)salicylaldehyde 
• 5351-69-9 4-Phenyl-3-thiosemicarbazide 

Relevant academic research and scientific papers

Triple Action Sensing Behaviour of a Single Receptor for the Detection of Multiple Analytes via Different Approaches

The thiosemicarbazide based receptor was synthesized with 4-(diethylamino)salicylaldehyde and N- phenyl-thiosemicarbazide by the simple condensation method and the properties were studied under the naked eye, UV-Vis and fluorescence studies etc. The synthesized receptor detects cyanide, cobalt, and mercury in acetonitrile medium. The observed color changes included colourless to yellow for cyanide, colourless to green for cobalt and colourless to yellow for mercury which were seen under naked eye without the aid of any instruments. Furthermore, the cyanide bound receptor detects Cr3+ by the relay recognition method. The detection limit of receptor with cyanide, cobalt & mercury was found to be 5.8 × 10? 7?M, 3.6 × 10? 7?M and 8.1 × 10? 7?M respectively. Experimental results were verified by DFT calculations. Receptor was successfully employed in the construction of INHIBIT and IMPLICATION logic gates. Graphical Abstract: [Figure not available: see fulltext.]

Probing 4-(diethylamino)-salicylaldehyde-based thiosemicarbazones as multi-target directed ligands against cholinesterases, carbonic anhydrases and α-glycosidase enzymes

With the fading of ‘one drug-one target’ approach, Multi-Target-Directed Ligands (MTDL) has become a central idea in modern Medicinal Chemistry. The present study aimed to design, develop and characterize a novel series of 4-(Diethylamino)-salicylaldehyde based thiosemicarbazones (3a-p) and evaluates their biological activity against cholinesterase, carbonic anhydrases and α-glycosidase enzymes. The hCA I isoform was inhibited by these novel 4-(diethylamino)-salicylaldehyde-based thiosemicarbazones (3a-p) in low nanomolar levels, the Ki of which differed between 407.73 ± 43.71 and 1104.11 ± 80.66 nM. Against the physiologically dominant isoform hCA II, the novel compounds demonstrated Kis varying from 323.04 ± 56.88 to 991.62 ± 77.26 nM. Also, these novel 4-(diethylamino)-salicylaldehyde based thiosemicarbazones (3a-p) effectively inhibited AChE, with Ki values in the range of 121.74 ± 23.52 to 548.63 ± 73.74 nM. For BChE, Ki values were obtained with in the range of 132.85 ± 12.53 to 618.53 ± 74.23 nM. For α-glycosidase, the most effective Ki values of 3b, 3k, and 3g were with Ki values of 77.85 ± 10.64, 96.15 ± 9.64, and 124.95 ± 11.44 nM, respectively. We have identified inhibition mechanism of 3b, 3g, 3k, and 3n on α-glycosidase AChE, hCA I, hCA II, and BChE enzyme activities. Hydrazine-1-carbothioamide and hydroxybenzylidene moieties of compounds play an important role in the inhibition of AChE, hCA I, and hCA II enzymes. Hydroxybenzylidene moieties are critical for inhibition of both BChE and α-glycosidase enzymes. The findings of in vitro and in silico evaluations indicate 4-(diethylamino)-salicylaldehyde-based thiosemicarbazone scaffold to be a promising hit for drug development for multifactorial diseases like Alzheimer's disease.

Caenorhabditis elegans as a model for exploring the efficacy of synthesized organoruthenium complexes for aging and Alzheimer's disease a neurodegenerative disorder: A systematic approach

The current article deals with the preparation and characterisation of new organoruthenium(II) complexes, namely [RuCp(Dea-Sal-tsc)(PPh3)] (1), [RuCp(Dea-Sal-mtsc)(PPh3)] (2), [RuCp(Dea-Sal-etsc)(PPh3)] (3) and [RuCp(Dea-Sal-ptsc)(PPh3)] (4). The new ruthenium(II) complexes were characterized by various analytical, spectral techniques. The structure of the ligand [H2-Dea-Sal-tsc] and the complex [RuCp(Dea-Sal-tsc)(PPh3)] (1) were confirmed by X-ray crystallography. The complexes (1–4) were used to study the toxicity, stress resistance, aging and neuro-protective effects by taking Caenorhabditis elegans as model. In?vitro free radical scavenging activity was performed by DPPH free radical scavenging assay, the complexes (1–4) exhibited highest scavenging activity than standard Vitamin C (IC50?=?5.28?±?0.10). The lifespan has increased over 22.4% in mev-1 mutant worms treated with complex 4. The complex 4 triggered the DAF-16 nuclear localization, increases sod-3 expression and reduced amyloid (Aβ) protein induced paralysis were observed. In the present study we confirmed that oxidative stress resistance of N2 and lifespan extension of mev-1 mutant which showed the potential ROS scavenging activity of complex 4. The results also confirmed the effective anti-aging potential of ruthenium complex 4 which may be developed as a therapeutic drug for the prevention of aging and age related neurodegenerative diseases. Further studies are required to find out the exact action of complex 4 on higher model.