Synthesis and Biological Activity of Allosteric Modulators of GABAB Receptors, Part 2. 3-(2,6-Bis-tert-butyl-4-hydroxyphenyl)propanols

2006 ◽  
Vol 59 (7) ◽  
pp. 457 ◽  
Author(s):  
David I. B. Kerr ◽  
Jabbar Khalafy ◽  
Jennifer Ong ◽  
Michael V. Perkins ◽  
Rolf H. Prager ◽  
...  
Keyword(s):  
Biological Activity ◽  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Tert Butyl

A series of 13 2,2-disubstituted 3-(3,5-di-t-butyl-4-hydroxyphenyl)propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABAB receptors. The activity (EC50, 4–7 μM) was greatest for the cyclohexyl and cyclopentyl analogues.

Synthesis and Biological Activity of Allosteric Modulators of GABAB Receptors, Part 1. N-(Phenylpropyl)-1-arylethylamines

2006 ◽  
Vol 59 (7) ◽  
pp. 445 ◽  
Author(s):  
David I. B. Kerr ◽  
Jennifer Ong ◽  
Michael V. Perkins ◽  
Rolf H. Prager ◽  
Ni Made Puspawati
Keyword(s):  
Biological Activity ◽  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators ◽  
Derivatives Of

A series of 15 analogues of fendiline, and 34 derivatives of N-(3-phenylpropyl)-1-arylethylamine have been prepared for evaluation as positive allosteric modulators of GABAB receptors. The most active (EC50, 10 nM) was N-(3,3-diphenylpropyl)-1-(3-chloro-4-methoxyphenyl)ethylamine 6g.

scholarly journals Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABAB receptors

2007 ◽  
Vol 17 (22) ◽  
pp. 6206-6211 ◽  
Author(s):  
Sébastien Guery ◽  
Philipp Floersheim ◽  
Klemens Kaupmann ◽  
Wolfgang Froestl
Keyword(s):  
Gabab Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators

scholarly journals Synthesis of alkyl derivatives of 3,7,10-trioxo-2,4,6,8,9,11-hexaaza[3.3.3]propellane and evaluation of their biological activity

2021 ◽  
Vol 101 (1) ◽  
pp. 19-26
Author(s):  
А.А. Sinitsyna ◽  
◽  
S.G. Il’yasov ◽  
Keyword(s):  
Biological Activity ◽  
Influenza A ◽  
Bacillus Pumilus ◽  
Maximum Yield ◽  
Methyl Derivative ◽  
Tert Butyl ◽  
Alkyl Derivatives ◽  
Derivatives Of ◽  
And Staphylococcus Aureus ◽  
Moderate Yield

Today 3,7,10-trioxo-2,4,6,8,9,11-hexaaaza[3.3.3]propellane (THAP) has not yet received widespread re-search attention due to the complexity of the synthesis. This work is devoted to the development of a method for the THAP derivatives synthesis, as well as to the study of their biological activity in comparison with al-kyl-substituted glycolurils (subject of comparison). ТНАРwas N-alkylated to furnish novel hexaalkyl deriva-tives of ТНАРwith methyl, ethyl and propyl substituents. The conditionsfor obtaining the maximum yield of the target productwere optimizedon the base of methyl derivative. The reaction proceeded in DMSO/КОНat 75–80ºC for 13hours in a moderate yield of 56%. The ethyl and propyl derivatives of ТНАРwere synthe-sized under the same conditions. The biological activity of the obtained ТНАРalkyl derivatives and glycoluril alkyl derivatives was evaluated against Sporosarcina ureae, Bacillus pumilus, Salmonella typhimurium and Staphylococcus aureus bacteria and influenza A virus. All the samples were found to exhib-it antibacterial activity against Staphylococcus aureus.It was shown that 2,4,6,8,9,11-hexapropyl-ТНАР, di-tert-butyl-diphenyl-, di-tert-butyl-dibenzyl-, di-tert-butyl-dimethyl-and di-isopropyl-dibenzylglycoluril, have exhibited also toxicity to living cells besides antiviral activity

scholarly journals Comparative Assessment of the Phytochemical Composition and Biological Activity of Extracts of Flowering Plants of Centaurea cyanus L., Centaurea jacea L., and Centaurea scabiosa L.

Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1279
Author(s):  
Natalia Sharonova ◽  
Evgeny Nikitin ◽  
Dmitriy Terenzhev ◽  
Anna Lyubina ◽  
Syumbelya Amerhanova ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Biological Activity ◽  
Plant Extracts ◽  
Ethanol Extract ◽  
Methyl Tert Butyl Ether ◽  
Butyl Ether ◽  
Tert Butyl ◽  
Phytochemical Composition ◽  
Centaurea Cyanus ◽  
Centaurea Jacea

The data on the phytochemical composition and biological activity for flowering plant extracts of the genus Centaurea (Knapweed)—cornflower (Centaurea cyanus L.), brown knapweed (Centaurea jacea L.), and greater knapweed (Centaurea scabiosa L.), which are typical representatives of the flora in the middle belt of the Russian Federation, were obtained. For the first time, biologically active substances such as pyranone, coumaran (2,3-dihydrobenzofuran), and 5-hydroxymethylfurfural were identified in ethanol and methanol extracts of Centaurea scabiosa L. by gas chromatography–mass spectrometry. Catechol and α-amyrin were the major components of the ethanol extract from Centaurea cyanus L., and flavone was the major component of Centaurea jacea L. flower extract. The greatest antimicrobial activity against phytopathogens was detected in Centaurea scabiosa L. when extracting freshly harvested flower biomass with methyl tert-butyl ether at room temperature: the minimum inhibitory concentrations were 60–120 µg/mL, the minimum fungicidal concentration was 120 µg/mL, and the minimum bactericidal concentration was 250 µg/mL. The low antioxidant activity of the studied plant extracts was established using the maximum values of Centaurea jacea L. Ethanol extract of Centaurea cyanus L. flowers had low antimicrobial and antioxidant activity. The extracts showed no phytotoxicity to garden cress germination but inhibited the growth of juvenile plants, especially roots. The greatest phytotoxic effect was revealed with methyl tert-butyl ether, where the depression of growth indicators was 35% or more.

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands

2018 ◽  
Vol 152 ◽  
pp. 223-234 ◽  
Author(s):  
Katarzyna Szczepańska ◽  
Tadeusz Karcz ◽  
Szczepan Mogilski ◽  
Agata Siwek ◽  
Kamil J. Kuder ◽  
...  
Keyword(s):  
Biological Activity ◽  
Tert Butyl ◽  
Piperazine Derivatives
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