6951-76-4Relevant academic research and scientific papers
Diaryl ethers with carboxymethoxyphenacyl motif as potent HIV-1 reverse transcriptase inhibitors with improved solubility
Fr?czek, Tomasz,Kamiński, Rafa?,Krakowiak, Agnieszka,Naessens, Evelien,Verhasselt, Bruno,Paneth, Piotr
, p. 9 - 16 (2018)
In search of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) with improved solubility, two series of novel diaryl ethers with phenacyl moiety were designed and evaluated for their HIV-1 reverse transcriptase inhibition potentials. All compounds exhibited good to excellent results with IC50 at low micromolar to submicromolar concentrations. Two most active compounds (7e and 7 g) exhibit inhibitory potency comparable or even better than that of nevirapine and rilpivirine. Furthermore, SupT1 and CD4+ cell infectivity assays for the most promising (7e) have confirmed its strong antiviral potential while docking studies indicate a novel binding interactions responsible for high activity.
A new supported reagent for the photochemical generation of radicals in solution
De Luca, Lidia,Giacomelli, Giampaolo,Porcu, Giancarlo,Taddei, Maurizio
, p. 855 - 857 (2007/10/03)
matrix presented A new polymer-supported radical source was developed by loading an N-hydroxy thiazole 2(3)-thione on a Wang resin. This new supported reagent can be employed for a solid-phase version of the Hunsdiecker reaction or to liberate free alkoxy radicals, in a variant of the "catch and release" technique, under very mild conditions (irradiation with a discharge lamp) and simplifying the purification procedure.
Piperazine derivatives, medicaments comprising these compounds, their use and processes for their preparation
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, (2008/06/13)
The present invention relates to piperazine derivatives of the general formula STR1 in which Ra, Y1 to Y3 and E are defined herein, tautomers thereof, stereoisomers thereof, including their mixtures, and salts thereof, and in particular physiologically tolerated salts thereof with inorganic or organic acids or bases. These compounds have valuable pharmacological properties, such as aggregation-inhibiting activity. This invention also relates to medicaments comprising these compounds and to processes for the preparation of these compounds.
Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
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, (2008/06/13)
Piperazine derivatives useful in the treatment or prevention of inflammation, bone degradation, thrombosis and tumor metastasis. Exemplary species are: (a) ?4-trans-?3-?4-(4-Pyridyl)-piperazin-1-yl!propionyl!amino!-cyclohexanecarboxylic acid, (b) 3-?4-trans-?4-(4-Pyridyl)-piperazin-1-yl!carbonylamino!-cyclohexylpropionic acid, (c) 3-?4-trans-?4-(4-Pyridyl)-piperazin-1-yl!malonylamino!cyclohexylcarboxylic acid, (d) Methyl ?4-trans-?3-?4-(4-pyridyl)-piperazin-1-yl!-propionyl!-amino!cyclohexane carboxylate, (e) Methyl 3-?4-trans-?4-(4-pyridyl)-piperazin-1-yl!-carbonylamino!cyclohexyl propionate, (f) Methyl ?4-trans-?4-(4-pyridyl)-piperazin-1-yl!-malonylamino!-cyclohexyl carboxylate, (g) Cyclohexyl ?4-trans-??4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate, and (h) Isobutyl ?4-trans-??4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate.
