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Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease.
Bioorg Med Chem
August 2021
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address:
A novel series of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues were designed and synthesized as H receptor antagonism based multitarget-directed ligands (MTDLs) for AD therapy using pharmacophore-combine strategy. The 2-styryl-5-hydroxy-4-pyrone pharmacophore with metal ion chelation, antioxidation, and Aβ aggregation inhibition activities was employed as the "eastern part", and a typical phenoxyalkylamine moiety was used as "central ring + western part" of the H receptor antagonist. The biological evaluation revealed that the majority of the target compounds demonstrated desirable multiple functions.
View Article and Find Full Text PDFOptimization and preclinical evaluation of novel histamine Hreceptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives.
Bioorg Med Chem
December 2018
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. Electronic address:
As a continuation of our search for novel histamine H 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 H receptors (hHR). In vitro test results proved the 4-pyridylpiperazine moiety as crucial element for high hHR affinity (hHR K = 5.
View Article and Find Full Text PDFSynthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HR ligands.
Eur J Med Chem
May 2018
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. Electronic address:
As a continuation of our search for novel histamine H receptor ligands, a series of twenty four new tert-butyl and tert-pentyl phenoxyalkylamine derivatives (2-25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer were evaluated for their binding properties at human histamine H receptor (hHR). The highest affinities were observed for 4-pyridyl derivatives 4, 10, 16 and 22 (K = 16.
View Article and Find Full Text PDFSynthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine HR ligands.
Bioorg Med Chem
May 2017
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. Electronic address:
As a continuation of our search for novel histamine H receptor ligands a series of twenty new tert-amyl phenoxyalkylamine derivatives (2-21) was synthesized. Compounds of four to eight carbon atoms spacer alkyl chain were evaluated on their binding properties at human histamine H receptor (hHR). The highest affinities were observed for pentyl derivatives 6-8 (K=8.
View Article and Find Full Text PDFNovel phenoxyalkylamine derivatives. VII. Synthesis and pharmacological activities of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives.
Chem Pharm Bull (Tokyo)
June 1992
Central Research Laboratory, Hokuriku Seiyaku Co., Ltd., Fukui, Japan.
To find a novel alpha-blocker with high alpha-blocking selectivity against dopamine D2-receptor affinity, we performed structural modification of the alkylene chains and the substituents on two benzene rings of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives. The modification of the alkylene chain between the amino moiety in the center of the molecule and the benzene ring (ring A) was found to be the most significant. 5-[2-[[2-(5-Fluoro-2-methoxyphenoxy)ethyl]amino]propyl]-2- methoxybenzenesulfonamide (II-4), which possesses 1-methylethyl as the alkylene chain, exhibited high alpha-blocking selectivity as well as potent alpha-blocking activity.
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