3524-86-5Relevant articles and documents
Optimization and preclinical evaluation of novel histamine H3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives
Szczepańska, Katarzyna,Karcz, Tadeusz,Kotańska, Magdalena,Siwek, Agata,Kuder, Kamil J.,Latacz, Gniewomir,Mogilski, Szczepan,Hagenow, Stefanie,Lubelska, Annamaria,Sobolewski, Micha?,Stark, Holger,Kie?-Kononowicz, Katarzyna
, p. 6056 - 6066 (2018)
As a continuation of our search for novel histamine H3 receptor ligands, a series of new acetyl and propionyl phenoxyalkylamine derivatives (2–25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer, composed of six various 4N-substituted piperazine moieties were evaluated for their binding properties at human histamine H3 receptors (hH3R). In vitro test results proved the 4-pyridylpiperazine moiety as crucial element for high hH3R affinity (hH3R Ki = 5.2–115 nM). Moreover introduction of carbonyl group containing residues in the lipophilic part of molecules instead of branched alkyl substituents resulted in increased affinity in correlation to previously described series, whereas propionyl derivatives showed slightly higher affinities than those of acetyl (16 and 22 vs. 4 and 10; hH3R Ki = 5.2 and 15.4 nM vs. 10.2 and 115 nM, respectively). These findings were confirmed by molecular modelling studies, demonstrating multiple ligand-receptor interactions. Furthermore, pharmacological in vivo test results of compound 4 clearly indicate that it may affect the amount of calories consumed, thus act as an anorectic compound. Likewise, its protective action against hyperglycemia and the development of overweight has been shown. In order to estimate drug-likeness of compound 4, in silico and experimental evaluation of metabolic stability in human liver microsomes was performed.
Design, synthesis, and anti-proliferative evaluation of 1: H -1,2,3-triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates in estrogen responsive and triple negative breast cancer cells
Awolade, Paul,Cele, Nosipho,Gu, Liang,Kaur, Mandeep,Kumar, Vipan,Pillay, Ruvesh Pascal,Sharma, Bharvi,Singh, Parvesh
, p. 11137 - 11147 (2020/07/15)
A series of 1H-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and in vitro evaluated against estrogen responsive (MCF-7) and triple negative (MDA-MB-231) breast cancer cells. Comparative analysis reve
Propargylamine derivative and synthesis method thereof
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Paragraph 0037-0041, (2020/06/16)
The invention discloses a series of propargylamine derivatives and a synthesis method thereof. The synthesis method of the derivative mainly comprises the following steps: (1) putting any one of the structures shown in the following formulas (A)-(E) and e
