Triazoles are heterocyclic compounds which have a five-membered ring of two carbon atoms and three nitrogen atoms. These structures have been interest in the development of novel compounds with anticonvulsant, antidepressant, antioxidant, anti-inflammatory, analgesic, antinociceptive, antibacter...
A new mechanism has been recently proposed, whereby melatonin may participate in the ongoing process of neuronal degeneration in models of neurodegenerative disorders, such as Parkinson's disease (PD). Antagonism of the melatonin receptor in rats using constant light or pinealectomy induced...
Mulberry fruit, which has been long used in traditional oriental medicine, was reported to ameliorate motor dysfunction and dopaminergic neuronal degeneration via antioxidant and antiapoptotic effects in an animal model of Parkinson's disease (PD). More than 95% of PD patients exhibit nonmo...
A group of 4-[2-(4-methyl(amino)sulfonylphenyl)-5-trifluoromethyl-2H-pyrazol-3-yl]-1,2,3,6-tetrahydropyridines (11–14) possessing a variety of substituents (Me, CO2Et, H, N = O) attached to the 1,2,3,6-tetrahydropyridyl N1-nitrogen atom were synthesized and evaluated as anti-inflammatory agents...
An irreversible parkinsonian-like movement disorder has been described in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and methcathinone (ephedrone) abusers. MPTP damages mitochondrial respiration, stimulates formation of reactive oxygen species, and contributes to apoptotic cell death in...
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure–activity relationships were develop...
We have shown that a 4-phenyl-1,2,3,6-tetrahydropyridine fragment plays an important role in improving inhibitory potency against poly(ADP-ribose) polymerase-1 (PARP-1). Various benzamide analogues linked with this fragment via alkyl spacers have been prepared and evaluated. As a result, some of...
The treatment of alkyl or aryl halides with an excess of tetrakis(pyridine)lithium tetrakis(N-dihydropyridyl)aluminate affords the corresponding 3-substituted-1,2,3,6-tetrahydropyridines in moderate to good yields via a tandem alkylation–reduction reaction.
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a well-known neurotoxicant that can selectively destroy dopaminergic neurons and MPTP-treated animals are often used as models for studying aspects of Parkinson’s disease (PD). While apoptosis has been suggested as a possible mechanism unde...
Parkinson's disease (PD) is a progressive neurodegenerative disorder accompanied by movement deficits with selective degeneration of dopaminergic neurons in the substantia nigra (SN). Recent studies indicate that early diagnosis of PD has important implications for the disease-modifying str...
BackgroundThe effects of chemical products on the nervous system have been studied by various scientists. In this work, the antiparkinsonian action of a water-soluble form of harmine hydrochloride was studied. The present studies aim to research antiparkinsonian action of the harmine hydrochlori...
Four derivatives of 9,10-bis[2-(2-alkoxynaphthalen-1-yl)vinyl]anthracene (BNAs) were designed, successfully synthesized and characterized by spectrofluorometer, powder wide-angle X-ray diffraction (PXRD) and differential scanning calorimetry experiments (DSC), etc. It was found that these compou...
Coupling reactions of 9,10-di(lithioethynyl)anthracene with dichloromono-, di-, and trisilanes, Cl(SiR2)mCl (m=1–3) gave polymers composed of alternating 9,10-diethynylanthracene and organosilicon units. With dichlorotetraorganodisilanes, the corresponding dianthracenophanes composed of two 9,1...
Three new cocrystals based upon 2,2′-diamino-4,4′-bis(1,3-thiazole) (DABTZ) with 4,4′-bipyridine (4,4′-bipy), 1,2-bis(4-pyridyl)ethylene (bpe) and 1,3-bis(4-pyridyl)propane (bpp): [(DABTZ) (4,4′-bipy)], [(DABTZ) (bpe)] and [(DABTZ) (bpp)] have been synthesized and characterized by elemental...
A superior synthetic route to 4,4′-diamino-2,2′-bipyridine has been developed. This procedure compares favorably with existing methods, producing 4 times the yield previously reported. In addition, mild reaction conditions are utilized, allowing a considerably more efficient production, and su...
A novel metal-free transannulation reaction of readily available N,3-diaryloxirane-2-carboxamides has been demonstrated as a simple efficient route to 3-arylquinolin-2(1H)-ones. The reaction involves one-pot acid-catalyzed Meinwald rearrangement and intramolecular Friedel–Crafts alkylation proc...
The ‘on-water’ generation of carbonyl ylide dipoles from diazoamides in the presence of rhodium(II) acetate dimer as the catalyst was demonstrated for the first time to synthesize spiroindolo-oxiranes and -dioxolanes. Unusual generation of carbonyl ylides with aromatic aldehydes having electro...
Chemical fixation of CO2 into the organic molecules is very challenging from the perspective of greenhouse gas consumption and manufacturing of chemicals with C1 backbone. The process was developed with the synthesis of an efficient polystyrene functionalized Magnesium-anthranilic acid complex (...
A palladium-catalysed reaction of conjugated enyne oxiranes with organoboron reagents is described. This method allows aryl-substituted vinylallenes containing a hydroxyl group on the allylic position to be synthesized, with good diastereomeric ratios, under mild conditions.
In the presence of a halobenzene or benzonitrile, Pseudomonas T-12 can produce substituted catechols from the corresponding substituted benzenes. A variety of monosubstituted benzenes with substituents containing up to four carbons, and some meta- and para- disubstituted benzenes, can serve as c...
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