Three new coordination compounds containing 5‑diethylamino‑2‑((4‑(phenyldiazenyl) phenylimino) methyl) phenol ligand have been synthesized and fully characterized. Single crystal structure showed that the ligand shows multiple coordination mode and the phenyl group next to azo group could rotate...
An efficient one-pot synthesis of 3-((aryl)(diethylamino)methyl)-4-hydroxy-2H-chromen-2-one derivatives has been developed from diethyl amine, aromatic aldehyde and 4-hydroxy coumarin via Mannich type reaction in the presence of Bi(NO3)3·5H2O. Also, the reaction of arylaldehyde, 4-hydroxy couma...
Thousands of death in Africa and other developing nations are still attributed to trypanosomiasis. Excessive sleep has been associated with increased inflammation. We report herein, the synthesis, antitrypanosomal and anti-inflammatory activities of eight new carboxamide derivatives bearing subs...
A series of iminothiazolidinone-sulfonamide hybrids (2a-k) was synthesized by heterocyclization of sulfanilamide thioureas with methyl bromoacetate and characterized by spectroscopic techniques, mass and elemental analysis. The synthesized derivatives were screened against four relevant human (h...
We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound of the series (1) displays significant anti-proliferative and cytotoxic activities against a panel of cancer cell lines, either se...
Structure–activity relationships (SAR) in 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide (FH535) were examined as part of a program to identify agents that inhibit the Wnt/β-catenin signaling pathway that is frequently upregulated in hepatocellular carcinoma (HCC). FH535 was reporte...
The synthesis, characterization and biological evaluation of series of cyclic imides incorporating the 4-sulfamoylbenzamide scaffold (16–29) is disclosed. The compounds were designed by application of the “tail approach” to the aromatic sulfonamide scaffold and prepared by reacting the proper...
As a part of our ongoing efforts towards developing novel carbonic anhydrase inhibitors based on the isatin moiety, herein we report the synthesis and biological evaluation of novel sulfonamides (5a-h, 10a-g and 11a-c) incorporating substituted 2-indolinone moiety (as tail) linked to benzenesulf...
N-Benzyl-N-(4-phenoxyphenyl)benzenesulfonamide derivatives were developed as a novel class of nonsteroidal glucocorticoid receptor (GR) modulators, which are promising drug candidates for treating immune-related disorders. Focusing on the similarity of the GR and progesterone receptor (PR) ligan...
A series of polycyclic imides was prepared by reaction of the benzenesulfonamide with an appropriate polycyclic acid anhydride in refluxing glacial acetic acid. The synthesized mono- and bis-sulfonamides were evaluated as a carbonic anhydrase inhibitors (CA, EC 4.2.1.1), more precisely against t...
Bait applications are frequently utilised to control the Mediterranean fruit fly, Ceratitis capitata (Wiedemann), because they can be applied rapidly and have a limited impact on natural enemies. However, the preferred toxicant, malathion, sometimes results in unacceptable residues and resistanc...
Malathion (MLT) is diethyl 2-[(dimethoxyphosphorothioyl) sulfanyl] butanedioate and one of the oldest and probably worldwide heavy used insecticides of the organophosphate family. There is evidence of acute and chronic toxicity, genotoxicity as well as carcinogenicity. The most critical tumors i...
A convenient and sensitive spectrophotometric methods was proposed for determination of Malathion (Mala) using Erythrosin B (EryB) as a probe through the Resonance Rayleigh scattering (RRS) technique. The interaction between EryB, Pd2+and malathion in the system was investigated by fluorescence,...
A highly sensitive dual-signal aptamer sensor based on polydopamine-gold nanoparticles (PDA-AuNPs) and exonuclease I (Exo I) was developed for detection of malathion. Compared with traditional sensing elements, aptamer has many advantages, such as high affinity, superior specificity, strong stab...
Effects of sub-lethal concentrations (0 (control), 0.009, 0.014, and 0.023 ppm) of the organophosphate insecticide “malathion” to rainbow trout (Oncorhynchus mykiss) after the determination of LC50-96 h value (0.093 ppm) were evaluated. Changes in biomarkers of neurotoxicity (acetylcholinester...
Malathion, one of commonly used organophosphate insecticides, has a wide range of toxic actions in different models. However, the effect of this compound on Ca2+ homeostasis and its related cytotoxicity in glial cells is elusive. This study examined whether malathion evoked intracellular Ca2+ co...
Malathion is a wide spectrum organophosphorothionate insecticide that is frequently found in drinking water, food and foodstuffs. Ovarian granulosa cells modulate oogenesis by providing metabolic nutrients to oocytes. They can decide the fate of folliculogenesis and oocyte maturation by supplyin...
ObjectivesMalathion is a widely used pesticide in the Kingdom of Saudi Arabia against pests that infest dates, and it causes severe damage to humans and animals. We evaluated the possible defensive effect of dietary supplementation with powdered black seeds (PBS) and powdered thyme leaves (PTL) ...
The present manuscript deals with the preparation of conducting polymer poly-3,4 ethylenedioxythiophene (PEDOT) and carbon nanomaterials such as carboxylated multi-walled carbon nanotubes (c-MWCNTs) based aptasensor for the detection of malathion organophosphate (OP). For the development of an a...
In drinking water treatment, complete mineralization of organophosphorus pesticides (OPPs) by UV-based advanced oxidation processes (UV AOPs) is rarely achieved. The formation of intermediate oxidation byproducts would likely have some profound effects on toxicity of the reaction solutions. This...
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