Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5-HTP induced head twitches (5-HT2A antagonism) and catalepsy studies in ...
Sushil Kumar, A. K. Wahi, Ranjit Singh
doaj +2 more sources
Photocatalysis and Kinetic Resolution by Lithiation to Give Enantioenriched 2-Arylpiperazines. [PDF]
Piperazines are important heterocycles in drug compounds. We report the asymmetric synthesis of arylpiperazines by photocatalytic decarboxylative arylation (metallaphotoredox catalysis) then kinetic resolution using n-BuLi/(+)-sparteine. This gave a range of piperazines with very high enantioselectivities.
Das A, Choi A, Coldham I.
europepmc +4 more sources
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
Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives [PDF]
Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to ...
DEANA ANDRIC +6 more
doaj +3 more sources
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
Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole [PDF]
Series of eight novel 5-substituted derivatives of benzimidazole were synthesized by condensation of corresponding diamine with ethyl-4-[4-(2-chlorophenyl)piperazin-1-yl] butanoate in refluxing 4N hydrochloric acid.
Vasić Vesna P. +5 more
doaj +1 more source
p38 mitogen‐activated protein kinase: Functions and targeted therapy in diseases
Our review provides an overview of the relationship between P38 mitogen‐activated protein kinase (p38MAPK) and disease, especially on small‐molecule inhibitors of four p38MAPK subtypes, and summarizes the challenges about the development of p38MAPK inhibitors.
Qinwen Zheng +10 more
wiley +1 more source
Easy access to several classes of heterocyclic compounds is provided by reacting 2‐cyanobenzaldehyde or 2‐acylbenzonitriles with a range of nucleophiles under mild conditions through divergent cascade reactions in an asymmetric way. Abstract 2‐Cyanobenzaldehye (also called 2‐formylbenzonitrile) and related 2‐acylbenzonitriles belong to a class of ...
Mohammad Sadeq Mousavi +2 more
wiley +1 more source
Investigation of antibacterial activity of cinnamyl derivatives of arylpiperazine [PDF]
The derivatives of cinnamic acid and N-arylpiperazine show antibacterial activity. In this work the potential synergistic effect of cinnamyl derivatives of arylpiperazine in selected bacteria was investigated. The antibacterial activities of the derivatives were evaluated against Gram-positive bacteria: Staphylococcus aureus ...
Irena Novakovic +5 more
openaire +3 more sources
Influence of N–1 substituent properties on binding affinities of arylpiperazines to the binding site of 5-HT1A receptor [PDF]
Serotonin receptors (5-HTRs), especially the 5-HT1A subtype, have been the subject of intensive research for the past decade, due to their function in human physiology.
MARIO V. ZLATOVIC +4 more
doaj +3 more sources

