Results 41 to 50 of about 629 (164)

Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF‐7 and MDA‐MB‐231

open access: yesJournal of Chemistry, Volume 2017, Issue 1, 2017., 2017
Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors.
Vincenza Barresi   +8 more
wiley   +1 more source

Hit‐To‐Lead Optimization of a Pyridylpiperazine Class Against Malaria: Pharmacokinetic Profile and In Vivo Efficacy of Optimized Compounds

open access: yesChemMedChem, Volume 21, Issue 13, 14 July 2026.
Chemical optimization of a novel pyridylpiperazine class yields two promising antimalarial candidates with an exceptional balance of metabolic stability and solubility. These optimized leads significantly protect mice from cerebral malaria, reducing parasitic load by up to 91.7%.
Douglas Davison da Silva Oliveira   +8 more
wiley   +1 more source

Synthesis of Some New Thiazole Derivatives and Their Biological Activity Evaluation

open access: yesJournal of Chemistry, Volume 2015, Issue 1, 2015., 2015
New 2‐(4‐arylpiperazine‐1‐yl)‐N‐[4‐(2‐(4‐substituted phenyl)thiazol‐4‐yl)phenyl]acetamide derivatives were synthesized and evaluated for their antimicrobial and anticholinesterase activities. Acetylcholinesterase inhibitory activities of the compounds were found weak contrary to expectations. It is unlikely that antifungal activity of the compounds was
Leyla Yurttaş   +4 more
wiley   +1 more source

Exemplary pharmacophore hypothesis selected for arylpiperazines with classical amide fragment.

open access: yes, 2013
Exemplary pharmacophore hypothesis selected for arylpiperazines with classical amide fragment mapping 6 out of 10 cluster representatives. The model fit 462 of the 533 compounds (87%) in the cluster. The feature abbreviations are: hydrogen-bond donor – D,
Stefan Mordalski (499181)   +6 more
core   +1 more source

Copper Complexes with Arylated Triethylenetetramine Ligands: Reactivity Toward Dioxygen and Peroxides

open access: yesEuropean Journal of Inorganic Chemistry, Volume 29, Issue 17, 17 June 2026.
Here, we describe new Cu(I)/Cu(II) complexes based on arylated tren ligands and investigate their reactivity toward O2 and peroxides. Low‐temperature–stopped flow studies revealed the formation of transient copper–oxygen species, including superoxido, hydroperoxido, and alkylperoxido intermediates.
Chiara Eleonora Campi   +2 more
wiley   +1 more source

Synthesis and Preliminary Pharmacological Evaluation of 2-[4-(Aryl substituted) piperazin-1-yl]-Nphenylacetamides: Potential Antipsychotics [PDF]

open access: yes, 2011
Purpose: Arylpiperazines have been recognized as the largest and most diverse class of compounds exerting actions on the central nervous system with strong affinity for serotonin and dopamine receptors.
Singh, R   +5 more
core   +4 more sources

Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry

open access: yesChemistryOpen, Volume 15, Issue 1, January 2026.
Piperazine‐based bioactive molecules represent a versatile class of compounds with broad therapeutic potential. Structural modification of the piperazine scaffold governs key structure–activity relationships, enabling antibacterial, antifungal, antitumor, neuroactive, and anti‐inflammatory activities.
Assel Ten   +5 more
wiley   +1 more source

Recent Advances in Isatin–Thiazole Hybrids: Synthesis, Structural Design, and Biological Application

open access: yesChemistry &Biodiversity, Volume 22, Issue 12, December 2025.
ABSTRACT Isatin–thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin–thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years ...
Isadora M. G. Andrade   +4 more
wiley   +1 more source

Microwave-Assisted Synthesis of Trazodone and Its Derivatives as New 5-HT1A Ligands: Binding and Docking Studies

open access: yesMolecules, 2019
Trazodone, a well-known antidepressant drug widely used throughout the world, works as a 5-hydroxytryptamine (5-HT2) and α1-adrenergic receptor antagonist and a serotonin reuptake inhibitor.
Jolanta Jaśkowska   +5 more
doaj   +1 more source

Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents

open access: yesChemMedChem, Volume 20, Issue 15, August 2, 2025.
The synthesis of a new series of 4,5‐dihydrothiazol‐2‐ylphenylpiperazine derivatives as serotoninergic ligands is described and tested for their affinity toward 5‐HT1A, 5‐HT2A,and 5‐HT2C and selected for further in vivo assays to determine their functional activity. The pharmacological studies highlight that among the developed derivatives, FG‐7 and FG‐
Giorgia Andreozzi   +18 more
wiley   +1 more source

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