Results 171 to 180 of about 40,506 (345)

Novel Potent and Selective Dopamine D4 Receptor Piperidine Antagonists as Potential Alternatives for the Treatment of Glioblastoma. [PDF]

open access: yesPharmaceuticals (Basel)
Matteucci F   +16 more
europepmc   +1 more source

Further Structure‐Activity Relationship of G Protein‐Gated Inwardly Rectifying Potassium Channels 1/2 Activators: Synthesis and Biological Characterization of In Vitro Tool Compounds

open access: yesChemMedChem, EarlyView.
Work presented here details the design and characterize novel G protein‐gated inwardly rectifying potassium channels (GIRK)1/2 activators. A new 4,4‐difluorocyclohexylpyrazole have been identified that confers improved potency and selectivity for GIRK1/2 versus GIRK1/4.
Sumaiya Nahid   +8 more
wiley   +1 more source

Chiron approaches to polyhydroxylated piperidines: promising glycosidase inhibitors

open access: yesARKIVOC, 2002
Dilip D. Dhavale   +3 more
doaj   +1 more source

Novel Para‐Phenylenediamine‐Based Derivatives as Receptor Tyrosine Kinase‐like Orphan Receptor 1 (ROR1) Inhibitors: An In Vitro Preliminary Characterization

open access: yesChemMedChem, EarlyView.
ROR1 represents a promising target for the development of novel antiproliferative compounds, giving its high expression in different cancer cell lines. The present study describes the workflow leading to the design, synthesis, and characterization of a series of para‐phenylenediamine‐based compounds able to interact with the target kinase, inhibiting ...
Gerardina Smaldone   +17 more
wiley   +1 more source

2-{<i>N</i>-[ω-(1-Benzylpiperidin-4-yl)alkyl]amino}-6-[(prop-2-yn-1-yl)amino]pyridine-3,5-dicarbonitriles Showing High Affinity for σ<sub>1/2</sub> Receptors. [PDF]

open access: yesInt J Mol Sci
Deuther-Conrad W   +7 more
europepmc   +1 more source

Intracellular and Extracellular Efficacy of Homoisoflavone Derivatives Against Mycobacterium tuberculosis: Progress Toward Novel Antitubercular Agents

open access: yesChemMedChem, Accepted Article.
Tuberculosis (TB) is the leading cause of death among infectious diseases, and new studies focusing new anti‐TB drugs are urgent due to the emergence of drug‐resistant strains. In this regard, homoisoflavones, an underexplored subgroup of flavonoids, were explored for their potential as anti‐TB agents.
Sanderson D. Calixto   +12 more
wiley   +1 more source

Synthesis and biological characterization of 4,4‐difluoro‐3(phenoxymethyl)piperidine scaffold as dopamine 4 receptor (D4R) antagonist in vitro tool compounds

open access: yesChemMedChem, Accepted Article.
We report the discovery and characterization of a novel series of 4,4‐difluoropiperidine etherbased dopamine D4 receptor antagonists. Structure‐activity relationship studies led to the identification of compound 14a, which displays exceptional binding affinity for the D4 receptor (Ki = 0.3 nM) and remarkable selectivity over other dopamine receptor ...
Saeedeh Saeedi   +3 more
wiley   +1 more source

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