In order to analyse further the discriminative stimulus properties of stimulant drugs, rats were trained to discriminate 2.0 mg/kg of dl-cathinone in a two-lever operant task. Dose-related generalization was seen to cathinone itself and to a wide range of stimulant drugs including d-amphetamine,...
Rats were trained to discriminate between the stimulus properties of 0.6 mg/kg l-cathinone and its vehicle in a two-lever, food-motivated operant task. Once trained, rats showed a dose-dependent decrease in discrimination performance with lower l-cathinone doses and analysis of the dose-response...
A series of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine derivatives were synthesized and their COX-1/COX-2 inhibitory activity as well as in vivo anti-inflammatory and analgesic effects were evaluated. All of compounds showed strong inhibition of COX-2 with IC50 values in the range ...
In order to overcome the capacity fading of LiNi1/3Co1/3Mn1/3O2/graphite lithium-ion batteries (LIBs) cycled in the voltage range of 3.0–4.6 V (vs. Li/Li+), di(methylsulfonyl) methane (DMSM) is evaluated as a new electrolyte additive. This study demonstrated that DMSM additive in the electrolyt...
The identification of novel PPAR ligands represents an attractive research to fully understand the complex biological pathways regulated by these receptors. Selective PPAR modulators, inverse agonists and antagonists of three PPAR isoforms could help to clarify biological effects on lipid and gl...
Recently we described a novel class of imidazopyridine compounds that showed exceptional anti-RSV potency in cell culture. However, unfavorable pharmacokinetic (PK) properties and glutathione (GSH) adduct liabilities impeded their further development. In a bid to address the PK and early safety ...
The molecule, 4-(Methylsulfonyl)piperazin-1-ium 2,4,6-trinitrophenolate is crystallized in the monoclinic crystal system under space group P21/c and with unit cell parameters a = 6.951(5) Å, b = 21.915(16) Å, c = 11.566(7) Å, β = 110.9(3)° and Z = 4. The crystal and molecular structure of the ...
Evidence that persistent environmental pollutants may target the male reproductive system is increasing. The male reproductive system is regulated by secretion of testosterone by testicular Leydig cells, and perturbation of Leydig cell function may have ultimate consequences. 3-Methylsulfonyl-DD...
The solid-liquid equilibrium for 1-methyl-4-(methylsulfonyl)benzene in nine solvents (methanol, ethanol, acetonitrile, ethyl acetate, acetone, N,N-dimethylformamide, n-butanol, n-propanol, isopropanol) were determined at temperatures from 278.15 K to 318.15 K by using the isothermal saturation m...
A series of novel 4 and 5-substituted methylsulfonyl benzothiazole (MSBT) compounds having amide, alkoxy, sulfonamide, nitro and amine functionality were synthesized from sequential reactions on 5-ethoxy-2-(methylsulfonyl)benzo[d]thiazole such as nitration, reduction, sulfonation, dealkylation, ...
DFP, a highly selective and potent COX-2 inhibitor, has been synthesized by a modified approach. Three modifications of the existing method enabled us to prepare DFP in good quantity.
Herein, we report on the identification of three potent glycine and related amino acid-based series of FXa inhibitors containing a neutral P1 chlorophenyl pharmacophore. A X-ray crystal structure has shown that constrained glycine derivatives with optimized N-substitution can greatly increase hy...
Asymmetric synthesis of a chiral cyclopentadiene (98% ee) was realized for the first time by palladium-catalyzed asymmetric allylation of sodium cyclopentadienide in dioxane. The cyclopentadiene was readily converted into chiral metallocenes of iron, zirconium, and titanium, whose enantiomeric e...
The effects have been quantified of t-butyl substituents on the thermodynamic stability of cyclopentadienide ions with no, one, two, and three t-butyl groups, 1−, 2−, 3− and 4−, respectively. The stability estimated from oxidation potential values decreases in the order 1− (+ 0.04 V) >2− (− 0.16...
Organometallic coordination chemistry is dominated by the pervasive cyclopentadienide (Cp−) ligand and its benzannulated derivatives indenide (Ind−) and fluorenide (Flu−). However, in the past decades a diverse coordination chemistry involving higher benzannulated homologues has developed. In th...
The heavy analogues of the anionic 6π-electron systems, lithium 1,2-disila-3-germacyclopentadienide 2− · [Li+(thf)], 1,2-disila-3,4-digerma- and 1,2,3,4-tetrasilacyclobutadiene dianions 72− · 2[K+(thf)2] and 82− · 2[K+(thf)2], were synthesized by the reduction of the neutral precursors 1, 3 ...
A series of alkali metal cyclopentadienides, amides, alkoxides and phenoxides was characterized using NMR spectroscopy in deuterated dimethyl sulfoxide. Deuterated dimethyl sulfoxide showed very good stability and solubility for these compounds. Very nice and well resolved spectra were obtained ...
This work describes recent results from our research program aiming at the synthesis and evaluation of new compounds acting as potential anti-inflammatory drugs. A series of novel acyl-hydrazones bearing 2-aryl-thiazole moiety were synthesized by the condensation between derivatives of 4-[2-(4-m...
6-Hydroxybenzothiazole, 2-cyano-6-hydroxybenzothiazole, and 2-(6-hydroxy-2-benzothiazolyl)thiazole-4-carboxylic acid (dehydroluciferin) dramatically enhance light emission from the horseradish peroxidase conjugate catalyzed oxidation of luminol, isoluminol, N-(6-aminobutyl)-N-ethyl isoluminol, a...
A study on the corrosion inhibition of N80 steel in 0.5 M HCl acid with (S)‑6‑Phenyl‑2,3,5,6‑tetrahydroimidazo[2,1‑b] thiazole was undertaken by conducting electrochemical, weight loss, surface morphology, and FTIR measurements. The inhibition efficiency was found to exceed 95%. An excellent inh...
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