Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines [PDF]
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 +3 more sources
Prediction of overall in vitro microsomal stability of drug candidates based on molecular modeling and support vector machines. Case study of novel arylpiperazines derivatives. [PDF]
Other than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline.
Szymon Ulenberg +6 more
doaj +2 more sources
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 ...
Andrzej Bojarski +2 more
exaly +3 more sources
Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands [PDF]
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated.
Krzysztof Marciniec +8 more
doaj +2 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
Quantitative structure-retention relationship study of arylpiperazines by liquid chromatography and multivariate chemometric methods [PDF]
Cilj ove disertacije bilo je sistematsko proučavanje hromatografskog ponašanjaserije novosintetisanih arilpiperazina u uslovima planarne hromatografije, procenaretencionih podataka na osnovu multivarijantnih statističkih metoda i utvrđivanje vezeizmeđu ...
Trifković, Jelena
core +10 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

