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
A series of 1-aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as microtubule destabilizers were designed, synthesised and evaluated for anticancer activity.
Chao Wang +11 more
doaj +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
The synthesis of a series of new n-propyl and n-butyl chain containing 1-arylpiperazine derivatives of quinazolidin-4(3H)-one (7) 2-phenyl-2,3-dihydrophthalazine-1,4-dione (8) and 1-phenyl-1,2-dihydropyridazine-3,6-dione (9) as potential serotonin ...
Sijka Charakchieva-Minol +4 more
doaj +1 more source
4-Azatricyclo[5.2.2.02,6]undecane-3,5,8-triones as Potential Pharmacological Agents
A series of twenty six arylpiperazine and aminoalkanol derivatives of 4-azatricyclo[ 5.2.2.02,6]undecane-3,5,8-trione have been prepared. The synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells.
Marta Struga +5 more
doaj +1 more source
A NEW SCAFFOLD FOR D3 DOPAMINERGIC AFFINITY CONTAINING ARYLPIPERAZINE FRAGMENT: MOLECULAR MODELING, SYNTHESIS, IN VITRO AND IN VIVO PHARMACOLOGICAL EVALUATION [PDF]
A new series of N-(6-substitutedbenzo[d]thiazol-2-yl)-2-(4-arylpiperazin-1-yl) acetamides (3a-f) and 2-(3-(4-arylpiprazin-1-yl)propylthio)benzo[d]thiazoles/-oxazoles/-imidazole (6a-f) wassynthesized by connecting arylpiperazine through a semi-rigid ...
Franziska U. Müller +1 more
doaj +1 more source
DESIGN AND SYNTHESIS OF A PIPERAZINE DERIVATIVE AS A HIGH AFFINITY 5-HTIA RECEPTOR LIGAND
Serotonin (5-HT) 1A receptors have been shown to have physiological, biochemical pharmacological and clinical values. The piperazino derivative 1 was rationally designed as a bulky, lipophilic N4-substituted arylpiperazine. Radioligand binding assay of 1
Mohamed El-Bermawy
doaj +1 more source
The absence of effective chronic treatment, expansion to non-endemic countries and the significant burden in public health have stimulated the search for novel therapeutic options to treat Chagas disease, a protozoan disease caused by Trypanosoma cruzi ...
Marina T. Varela +4 more
doaj +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
A perspective on multi‐target drug discovery and design for complex diseases
AbstractDiseases of infection, of neurodegeneration (such as Alzheimer's and Parkinson's diseases), and of malignancy (cancers) have complex and varied causative factors. Modern drug discovery has the power to identify potential modulators for multiple targets from millions of compounds.
Rona R. Ramsay +4 more
wiley +1 more source

