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2 article(s) from Bregestovski, Piotr

Azologization of serotonin 5-HT₃ receptor antagonists

Karin Rustler,
Galyna Maleeva,
Piotr Bregestovski and
Burkhard König

Beilstein J. Org. Chem. 2019, 15, 780–788, doi:10.3762/bjoc.15.74

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Scheme 1: Approach of the direct azologization of reported [60,61] serotonin 5-HT₃R antagonists via replacement of a...

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Scheme 2: Synthesis of the differently substituted quinoxaline azobenzene derivatives 5a and 5b via Baeyer [62]–M...

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Scheme 3: Synthesis of the methoxy-substituted quinoxaline derivative 12a via diazotization [66-69].

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Scheme 4: General procedure for the synthesis of purine- and thienopyrimidine-substituted arylazobenzenes and...

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Scheme 5: Synthesis of the thiomethyl-linked purine azobenzene 23 [62,63,72-74].

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Scheme 6: Synthesis of the amide-linked azobenzene purine 28 [62,63,75-77].

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Figure 1: UV–vis absorption spectra measured at 50 µM in DMSO. Left: purine derivative 16c; right: azo-extend...

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Figure 2: On the left panel representative traces of currents induced by the application of 3 µM 5HT (black t...

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Published 25 Mar 2019

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New GABA amides activating GABA_A-receptors

Peter Raster,
Andreas Späth,
Svetlana Bultakova,
Pau Gorostiza,
Burkhard König and
Piotr Bregestovski

Beilstein J. Org. Chem. 2013, 9, 406–410, doi:10.3762/bjoc.9.42

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Figure 1: The neurotransmitter GABA.

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Scheme 1: Synthesis of GABA-amide hydrochlorides 4a–c and 6a–f. (i) THF, reflux; (ii) MeOH, HCl (5%); (iii) T...

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Figure 2: Effect of 7b on GABA_A-receptor activation. (A) Superimposed traces of whole-cell currents induced b...

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Figure 3: Absence of GABA_A-receptor activation on application of 4c. Top traces: Examples of whole-cell curre...

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Figure 4: Variation of EC₅₀ values with the number n of methylene units separating the amide and the ammonium...

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Figure 5: Effect of 7d on GABA_A-receptor activation. (A,B) Superimposed traces of whole-cell currents induced...

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Published 20 Feb 2013

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Azologization of serotonin 5-HT3 receptor antagonists

New GABA amides activating GABAA-receptors

Azologization of serotonin 5-HT₃ receptor antagonists

New GABA amides activating GABA_A-receptors