Two focused libraries based on two types of compounds, that is, thiazolidinediones and dioxazaborocanes were designed. Structural resemblances can be found between thiazolidinediones and well-known furanone type quorum sensing (QS) inhibitors such as N-acylaminofuranones, and/or acyl-homoserine ...

A facile, convenient, and two step strategy for synthesis of spirooxindoles containing α-arylidene-γ-butyrolactone moiety has been developed via monoalkylation of 2-oxindoles with Baylis-Hillman acetates followed by the spirolactonization of the resulting cinnamic esters on treatment with phen...

The aim of this study was to investigate and characterize different crystal forms of arteether, a rapidly acting, highly potent antimalarial drug for the treatment of acute Plasmodium falciparum malaria. Six different crystal forms were prepared utilizing various polar and non-polar solvents. Sc...

Inoculation with live sporozoites under prophylactic antimalarial cover (CPS-immunization) represents an alternate approach to develop sterile, reproducible, and long-term protection against malaria. Here, we have employed arteether (ART), a semi synthetic derivative of artemisinin to explore it...

The study evaluates in vivo antimalarial activity of arteether and garlic pearl oil combination in Plasmodium berghei-infected mouse model of malaria. 72 h (Day 3) post infection, at 2–4% parasitemia, mice were treated with single dose intramuscular injection of α-β arteether, at 750 μg, in ...

The present study describes an easy and efficient approach for the removal of methyl p-toluenesulfonate, a potentially genotoxic impurity (GTI) from a model active pharmaceutical ingredient (API), 21-chlorodiflorasone. For this purpose, several polystyrene–divinylbenzene based and silica based ...

In this work, the aggregation behavior of 1-butyl-3-methylimidazolium p-toluenesulfonate (BmimTOS), a new type of cationic hydrotrope, was investigated, where two distinct inflection points C1 and C2 were reflected by the change of conductivity, micro-polarity, surface tension. Therefore, it is ...

Noncentrosymmetric crystal of Nicotinium p-Toluenesulfonate (NPT) was grown by slow evaporation growth method. The crystal structure was determined by Single crystal X-ray diffraction and it confirms that the grown NPT crystal belong to orthorhombic crystal system with noncentrosymmetric space g...

Aldose reductase has been purified to homogeneity from bovine retina. It has an apparent molecular weight of 32,000 daltons and shares immunological and kinetic properties with the much studied aldose reductases purified from various sources. Retinal aldose reductase displays aKmof approximately...

Lipid peroxidation and its end-product, 4-hydroxyhexenal (HHE), are known to affect redox balance during aging, which causes various degenerative processes including vascular alterations from endothelial cell deterioration. To better understand the molecular action of HHE in the development of v...

Cachexia, the most severe paraneoplastic syndrome, occurs in about 80% of patients with advanced cancer; it cannot be reverted by conventional, enteral, or parenteral nutrition. For this reason, nutritional interventions must be based on the use of substances possessing, alongside nutritional an...

4-Hydroxynonenal and 4-hydroxyhexenal are cytotoxic aldehydic products of lipid peroxidation with high biological activity. Peroxidation of n−6 fatty acids produces 4-hydroxynonenal, but the origin of 4-hydroxyhexenal has been uncertain. We now present evidence that 4-hydroxyhexenal is generated...

Multiple studies have demonstrated elevations of α, β-unsaturated aldehydes including 4-hydroxynonenal (HNE) and acrolein, in vulnerable regions of mild cognitive impairment (MCI), preclinical Alzheimer's disease (PCAD), and late stage Alzheimer's disease (LAD) brain. However, there ...

C-4 Fluorination of a series of 3,5-diarylisoxazoles has been accomplished using the N-F reagent Selectfluor®. With substrates containing neutral or activating substituents on the 5-phenyl ring, acetonitrile at room temperature or at reflux could be used as solvent. However, when deactivating su...

The halogenation of 3-arylimidazo[1,5-a]pyridines was carried out with iodine, bromine, N-chlorosuccinimide, and 1-fluoro-2,4,6-trimethylpyridinium tetrafluoroborate as halogenating agents to give selectively halogenated products 1-halo-3-arylimidazo[1,5-a]pyridines in good to excellent yields. ...

A series of beta-carbolines with other heterocycles linked by phenyl ring has been designed and synthesized. The key intermediates 3 and 5 were synthesized by condensing tryptamine and teraldehyde via Pictet- Spengler method. All the newly synthesized compounds were tested for their anticancer a...

A series of novel isocombretastatin A-4 (isoCA-4) analogs were designed and synthesized by replacing 3,4,5-trimethoylphenyl and isovanillin of isoCA-4 with quinoline and indole moieties, respectively. The structure activity relationships (SARs) of these synthesized quinoline-indole derivatives h...

Indole is a chemical from the decomposition of shrimp and is used extensively to indicate seafood freshness. US Food and Drug Administration (FDA) sets its concentration of

The Kabachnik–Fields condensation was extended using secondary phosphine oxides, such as dibenzylphosphine oxide and bis(4-methylphenyl)phosphine oxide as the P-reactant in reaction with formaldehyde and different primary amines. Besides the α-aminophosphine oxides, the corresponding bisproduc...

The asymmetric synthesis of homochiral (S)-(+)-ethyl 3-dimethylamino-3-phenyl propionate, via stereoselective Michael addition of lithium dimethylamide to (S)-Z-[(η5-C5H5)-Fe(CO)(PPh3)COCHCHPh] and oxidative decomplexation, establishes the absolute configuration of Winterstein's acid, 3-...