Results 31 to 40 of about 605 (157)
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
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
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
Exemplary pharmacophore hypothesis selected for arylpiperazines with classical amide fragment.
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
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
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
A Versatile and Practical Microwave-Assisted Synthesis of Sterically Hindered N-Arylpiperazines
A wide-ranging and practical synthesis of structurally diverse, sterically hindered N-arylpiperazines from 2,2′-(4-nitrophenylsulfonylazanediyl) bis(ethane-2,1-diyl) bis(4-nitrobenzenesulfonate) and substituted anilines has been achieved using microwave ...
Rong Gao (476219) +1 more
core +1 more source
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
Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry
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
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

