Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3
An effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3 was worked out on two different routes, both starting from enantiomerically pure cis‐2‐aminocyclohexanols. The absolute configuration of the more active enantiomer was elucidated. These chiral pool syntheses provide sufficient amounts of the enantiomerically pure
Katharina Kriegler +3 more
wiley +1 more source
Protective mechanism of arylpiperazine dopaminergic D2ligands on nitric oxide and 6-hydroxydopamine induced SH-SY5Y human neuroblastoma cell death [PDF]
U ovom radu je ispitivan uticaj 20 novosintetisanih arilpiperazinskihdopaminergičkih liganada na vijabilnost humanih SH-SY5Y neuroblastomskih ćelijatretiranih donorom azot monoksida (engl. nitric oxide, NO) natrijum nitroprusidom(engl.
Tovilović-Kovačević, Gordana
core +2 more sources
Neuroprotective arylpiperazine dopaminergic/serotonergic ligands suppress experimental autoimmune encephalomyelitis in rats [PDF]
Arylpiperazine-based dopaminergic/serotonergic ligands exert neuroprotective activity. We examined the effect of arylpiperazine D-2/5-HT1A ligands, N-{4-[2-(4-phenyl-piperazin-1-yl)-ethyl}-phenyl]- picolinamide (6a) and N-{3-[2-(4-phenyl-piperazin-1-yl ...
Trajković, Vladimir +27 more
core +1 more source
Interaction of Arylpiperazines with the Dopamine Receptor D2 Binding Site [PDF]
The docking of several 1-benzyl-4-arylpiperazines to the dopamine receptor (DAR) D2 was examined. The results demonstrated that the interaction of protonated N1 of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ring of the arylpiperazine part of the ligand with Phe 178 (VI.44), Trp 182 (VI.48) and Tyr 216 (VII.58)
Šukalović, Vladimir +5 more
openaire +4 more sources
Two new DTPA-bis(amide) based ligands conjugated with the arylpiperazinyl moiety were synthesized and subsequently transformed into their corresponding Gd(III) complexes 1 and 2 of the type [Gd(L)H2O]·nH2O.
Abdullah O. Ba-Salem +4 more
doaj +1 more source
6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluation [PDF]
Eight new compounds with halogen atom introduced into the benzimidazole- 2-thione dopaminergic pharmacophore of 5-[2-(4-arylpiperazin-1-yl)ethyl]-1,3-dihydro- 2H-benzimidazole-2-thiones with the arylpiperazine part of the molecule being selected ...
Andrić Deana +5 more
doaj +3 more sources
In Vitro and in Silico Analysis of the Residence Time of Serotonin 5-HT7Receptor Ligands with Arylpiperazine Structure: A Structure-Kinetics Relationship Study [PDF]
During the last decade, the kinetics of drug-target interaction has received increasing attention as an important pharmacological parameter in the drug development process.
Niso M. +8 more
core +2 more sources
Synthesis of I-arylpiperazine-4-thiocarboxamides [PDF]
The reaction of 1-arylpiperazine salts with hot aqueous ammonium thiocyanate for a short time affords only the thiocyanate salts. l-Arylpiperazine-4-thiocarboxamides have been obtained by prolonged heating of the aqueous solutions of the thiocyanate ...
Ghate, S. P. +3 more
core +1 more source
Synthesis of novel 2-(piperazino-1-yl-alkyl)-1H-benzimidazole derivates and assessment of their interactions with the D2 dopamine receptor [PDF]
A total of 14 novel arylpiperazines were synthesized, and pharmacologically evaluated by measuring their affinities towards the D2 dopamine receptor (DRD2) in a [3H]spiperone competition assay.
Penjišević Jelena Z. +5 more
doaj +1 more source
Neuroprotective properties of arylpiperazine-sulphonamides in in vitro models of Parkinson's disease [PDF]
Introduction: Parkinson’s disease (PD) is a neurodegenerative disease characterised by the degeneration of dopaminergic neurons in the substantia nigra.
Kingslake, Alice +2 more
core +1 more source

