Hydrocortisone, cortexolone, hydrocortisone-17-butyrate, and budesonide were oxidized into α-ketoaldehydes by air exposure in the presence of Cu(OAc)2. When free hydroxyl functions were present at position 17, hydrocortisone and cortexolone, the formed oxidation products, were identified as hem...

BackgroundAdipocyte dysfunction, obesity and associated metabolic disorders are of prime healthcare concern worldwide. Among available medications, natural products and inspired molecules hold 40% space in clinically prescribed medicines. In queue, this study overcomes the drawback of curcumin&#...

A novel series of indoles and 1H-pyrrolo[2,3-b]pyridines having a piperidine ring at the 3-position were synthesized and found to bind with high affinity to the ORL-1 receptor. Structure–activity relationships at the piperidine nitrogen were investigated in each series. Substitution on the phen...

(−)-6-[2-[4-(3-Fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone was identified as an orally active NR2B-subunit selective N-methyl-d-aspartate (NMDA) receptor antagonist. It has very high selectivity for NR2B subunits containing NMDA receptors versus the HERG-...

A new triphenylamine-based diamine monomer 4,4′-diamino-4″-(1-piperidinyl)triphenylamine was synthesized and polymerized with various aromatic dicarboxylic acids via the phosphorylation polyamidation technique leading to a series of redox-active aromatic polyamides (aramids). All the aramids e...

The electrophysiological effects of N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazolamine (R56865), a drug which protects heart cells from ischemia-induced arrhythmias, was studied on intracellularly-recorded CA1 neurons of the rat hippocampal slice under normal or hypoxic ...

Novel piperidinyl-based sulfamide derivatives were designed and synthesized through various synthetic routes. Anticancer activities of these sulfamides were evaluated by phenotypic screening on National Cancer Institute's 60 human tumor cell lines (NCI-60). Preliminary screening at 10 μM c...

Alzheimer's disease (AD) is a degenerative neurological disorder that causes progressive and irreversible loss of connections between brain cells and loss of mental functions.Clinical and postmortem studies show that the biochemical changes in brains of AD patients include decrease in acety...

AimN-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity.

This text presents complementary data corresponding to pharmacological and toxicological characterization of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA) compound. These data support our research article entitled “Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl...

Drugs used for the treatment of castration resistant prostate cancer (CRPC) include Abiraterone acetate (Zytiga®) and Enzalutamide (XTANDI®). However, these drugs provide clinical benefit in metastatic disease for only a brief period before drug resistance emerges. One mechanism of drug resistan...

The pharmacological properties of (±)-2-(N-tert-butylamino)-3′-iodo-4′-azidopropiophenone [(±)-SADU-3-72], a photoreactive analog of bupropion (BP), were characterized at different muscle nicotinic acetylcholine receptors (AChRs) by functional and structural approaches. Ca2+ influx results i...

The preparation and the pharmacological evaluation of the R- and S-isomers of 3-(2′-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 42) and 3-(3′-methyl-2′-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 44), two potassium channel openers, is described. Their...

The molecular and solid-state structures of methyl [2-(acridin-9-ylimino)-3-(tert-butylamino)-4-oxothiazolidin-5-ylidene]acetate (4) were determined by X-ray diffraction, 1H NMR, 13C NMR, CI mass spectroscopy and B3LYP calculations using the basis sets 6-31G(d, p), 6-311+G(d, p) and 6-311++G(2d,...

Photochemical degradation and relative toxicity reduction of agricultural wastewater contaminated with methyl 1-[(butylamino)carbonyl]-1H-benzimidazol-2-ylcarbamate (benomyl) by the sonophotocatalytic system was compared with that of the photocatalytic system. Under the optimal conditions, i.e.,...

5e-tert-Butyl-2e-[4-(substituted-ethynyl)phenyl]-1,3-dithianes with selected functional groups (R) on the ethynyl moiety are potent blockers of the GABA-gated chloride channel measured as inhibitor concentration (IC50) for 4-n-[3H]propyl-1-(4-ethynylphenyl)-2, 6,7-trioxabicyclo[2.2.2]octanebindi...

Palladium-catalyzed reactions of diastereomerically pure chiral 2-alkynyl p-toluenesulfinates under very mild reaction conditions gave both enantiomers of optically active sulfonyl allenes in good yields with high stereospecificity. The stereochemistry of this transformation with the assistance ...

The synthesis and Myers–Saito type cycloaromatization reactions of 10-membered enediynes containing a sulfone or a sulfoxide moiety are described. These enediynes cycloaromatized smoothly under physiological conditions to generate bioactive α,3-didehydrotoluene biradicals, that showed potent D...

A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -...

Synthesis of aryl biaryl sulfones 3 with good yields is described. The one-pot efficient synthetic route is carried by the NaH-mediated tandem [C3+C3] annulations of cinnamaldehydes 1 and propargylic sulfones 2 under the boiling THF conditions.