New chiral dioxidomolybdenum(VI) complexes with tridentate Schiff base ligands obtained by monocondensation of 1R,2S(−)-norephedrine with salicylaldehyde and its derivatives were synthesized. The complexes were characterized by elemental analysis and by their IR, CD, UV–vis, one- (1H) and two-d...

AbsractA series of novel pyridazinone derivatives bearing benzenesulfonamide moiety (2a–h) has been synthesized by the condensation of appropriate aroylacrylic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Five derivatives (2a, 2b, 2d, 2g and 2h) were evaluated for their anti...

A library of fluorescent molecular rotors (FMRs) were synthesized by condensation of 2-chloroimidazo[1,2-a]pyridine-3-carbaldehyde with various active methylene moieties and their viscosity sensing properties were studied. The substituted 2-chloroimidazo[1,2-a]pyridine-3-carbaldehydes were prepa...

The multi-component Betti reaction of 2-naphthol, benzaldehyde and (S)-amines, that usually provides highly valuable aminobenzylnaphthol bearing two stereogenic centers, yielded a completely racemic product, when (S)-valine methyl ester was employed as the amine in the usual reaction protocol. T...

Phenylazocarboxylic tert-butyl esters have recently been shown to be highly versatile building blocks due to their ability to undergo nucleophilic aromatic substitutions under mild conditions, particularly well with [18F]fluoride, and to act as precursors for aryl radicals. In this article, we n...

When administered to human subjects, nandrolone is metabolized into two main products, 19-norandrosterone (19-NA) and 19-noretiocholanolone (19-NE). Recent studies demonstrated the endogenous production of these compounds in man at concentrations very close to the threshold of the International ...

A method to quantify metabolites of 17β-nandrolone (17βN) in boar and horse urine has been optimized and validated. Metabolites excreted in free form were extracted at pH 9.5 with tert-butylmethylether. The aqueous phases were applied to Sep Pak C18 cartridges and conjugated steroids were elut...

Nandrolone decanoate administration and strenuous exercise increase the extent of renal damage in response to renal toxic injury. We studied the role played by oxidative stress in the apoptotic response caused by nandrolone decanoate in the kidneys of strength-trained male CD1 mice. To measure c...

Nandrolone, an anabolic steroid, is used for the treatment of several diseases and is available in various pharmaceutical formulations. The most widely used pharmaceutical formulation is Deca-Durabolin®, but other products, such as Keratyl® eye drops solution, are also currently administered.Nan...

19-Norandrostenedione (NAED) and nandrolone are anabolic-androgenic steroids (AASs). Nandrolone was regarded solely as a synthetic AAS until the 1980s when trace concentrations of apparently endogenous nandrolone were detected in urine samples obtained from intact male horses (stallions). Since ...

Novel series of N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides were discovered as potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitors. SAR studies of the RORγt HTS hit 6a led to identification of thiazole ketone amide 8h and thio...

A novel series of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as RORγt inverse agonists was discovered. Binding mode analysis of a RORγt partial agonist (2c) revealed by co-crystal structure in RORγt LBD suggests that the inverse agonists do not directly interfere with the interaction between H1...

Fifteen novel stilbene analogues containing thiazole moiety were designed and synthesized. The structure of the synthesized compounds was confirmed by 1H NMR, 13C NMR and ESI-HRMS. These compounds were screened for their topoisomerase I inhibitory activity using Top1-mediated relaxation assay, a...

The solubility of 2-chloro-3-(trifluoromethyl)pyridine was measured at 273.15 K–303.15 K under atmospheric pressure in methylbenzene, dichloromethane, ethanol, n-propanol, n-hexane, n-heptane and ethanol + 1-propanol binary solvents. The solubility of 2-chloro-3-(trifluoromethyl)pyridine in pur...

The possibility of co-crystallization of polyfluoroaromatic meta-diamines with 18-crown-6 in the 2:1 ratio was tested using a large group of substrates with various frameworks (benzene, naphthalene, and pyridine) and substituents (H, Cl, CF3). Co-crystals of 2:1 stoichiometry were obtained from ...

The activating effect of trifluoromethyl groups in 2-chloro(trifluoromethyl)pyridines was investigated by comparing reactions of these compounds and of 2-chloropyridine with secondary cyclic amines. The ammonolysis of 2-chloro-3-trifluoromethylpyridine and 2-chloro-4-trifluoromethylpyridine is a...

The 2-[18F]fluoro-3-pent-4-yn-1-yloxypyridine ([18F]FPyKYNE) analog of the potent non-peptide angiotensin II type 1 receptor (AT1R) blocker losartan was produced via click chemistry linking [18F]FPyKYNE to azide-modified tetrazole-protected losartan followed by TFA deprotection. Preliminary smal...

The 3-deaza analogs of the naturally occurring adenine-based carbocyclic nucleosides aristeromycin and neplanocin possess biological properties that have not been optimized. In that direction, this paper reports the strategic placement of a fluorine atom at the C-2 and C-3 positions and a methyl...

A simple method for pyridoxal structural modification via furan ring closure was developed resulting in 2-acyl- and 2-heteroarylfuro[2,3-c]pyridines. The reaction products can be proposed as pyridoxal mimetics to inhibit pyridoxal 5′-phosphate-dependent enzymes.

Glycosylation is promoted by acid promoters rendering the reactions with basic acceptors challenging. This report presents an in depth study involving methyl 6-(hydroxymethyl)picolinate as the model acceptor and 22 glycosyl donors to afford the desired glycosides in good yields ranging from 46% ...