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Search for "biologically active" in Full Text gives 549 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Discrimination of β-cyclodextrin/hazelnut (Corylus avellana L.) oil/flavonoid glycoside and flavonolignan ternary complexes by Fourier-transform infrared spectroscopy coupled with principal component analysis

  • Nicoleta G. Hădărugă,
  • Gabriela Popescu,
  • Dina Gligor (Pane),
  • Cristina L. Mitroi,
  • Sorin M. Stanciu and
  • Daniel Ioan Hădărugă

Beilstein J. Org. Chem. 2023, 19, 380–398, doi:10.3762/bjoc.19.30

Graphical Abstract
  • biologically active molecules on CD-coated polymers used in chromatography [62]. PCA was used for the evaluation of the similarity/dissimilarity of some pesticides, especially fungicides and herbicides, using the effect of a water-soluble β-CD polymer on the apparent pesticide’s lipophilicity [63]. Also
  • above-mentioned biologically active compounds and its content varies in complexes at 1:1:1 and 3:1:1 molar ratios. In the FTIR spectra of β-CD as a host, besides the wavenumbers corresponding to characteristic bands of β-CD, their intensities are relevant for the discrimination of the ternary complexes
  • thermal/oxidative stability of ternary complexes is similar to β-CD hydrate, as was evaluated by TG and DSC. Moreover, the formation of the molecular inclusion complexes is supported by thermal analysis (partial replacing of the hydration water by biologically active molecules and disappearance of the DSC
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Published 28 Mar 2023

Sequential hydrozirconation/Pd-catalyzed cross coupling of acyl chlorides towards conjugated (2E,4E)-dienones

  • Benedikt Kolb,
  • Daniela Silva dos Santos,
  • Sanja Krause,
  • Anna Zens and
  • Sabine Laschat

Beilstein J. Org. Chem. 2023, 19, 176–185, doi:10.3762/bjoc.19.17

Graphical Abstract
  • by a hydrozirconation/acylation sequence. Examples of biologically active compounds with (2Ε,4E)-unsaturated ketone units. Selected examples for the synthesis of conjugated dienones from the literature [6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21]. Previous work of hydrozirconations
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Published 17 Feb 2023

1,4-Dithianes: attractive C2-building blocks for the synthesis of complex molecular architectures

  • Bram Ryckaert,
  • Ellen Demeyere,
  • Frederick Degroote,
  • Hilde Janssens and
  • Johan M. Winne

Beilstein J. Org. Chem. 2023, 19, 115–132, doi:10.3762/bjoc.19.12

Graphical Abstract
  • [81]. Miglustat is a biologically active analog of the natural product deoxynojirimycin, and its enantiomer also shows a promising profile in early biological activity studies. In future applications of 1,4-dithiane or -dithiin building blocks, the recently described zincation protocol by Knochel and
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Published 02 Feb 2023

Revisiting the bromination of 3β-hydroxycholest-5-ene with CBr4/PPh3 and the subsequent azidolysis of the resulting bromide, disparity in stereochemical behavior

  • Christian Schumacher,
  • Jas S. Ward,
  • Kari Rissanen,
  • Carsten Bolm and
  • Mohamed Ramadan El Sayed Aly

Beilstein J. Org. Chem. 2023, 19, 91–99, doi:10.3762/bjoc.19.9

Graphical Abstract
  • -azidocholest-5-ene (5) in high yield. The same product was recently obtained by direct dehydroxyazidation of cholesterol upon treatment with N-acetyl azidobenziodazolone (ABZ) and PPh3 in THF [19], Table 1. While synthesizing new potential biologically active probes with cholesterol scaffolds in the Port Said
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Published 27 Jan 2023

NaI/PPh3-catalyzed visible-light-mediated decarboxylative radical cascade cyclization of N-arylacrylamides for the efficient synthesis of quaternary oxindoles

  • Dan Liu,
  • Yue Zhao and
  • Frederic W. Patureau

Beilstein J. Org. Chem. 2023, 19, 57–65, doi:10.3762/bjoc.19.5

Graphical Abstract
  • investigations revealed that this cyclization reaction proceeds via a cascade radical pathway. We expect these results to encourage the further development of NaI/PPh3-catalyzed and related synthetic methods. Representative natural products and biologically active molecules containing an oxindole moiety [7][8][9
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Published 16 Jan 2023

Digyalipopeptide A, an antiparasitic cyclic peptide from the Ghanaian Bacillus sp. strain DE2B

  • Adwoa P. Nartey,
  • Aboagye K. Dofuor,
  • Kofi B. A. Owusu,
  • Anil S. Camas,
  • Hai Deng,
  • Marcel Jaspars and
  • Kwaku Kyeremeh

Beilstein J. Org. Chem. 2022, 18, 1763–1771, doi:10.3762/bjoc.18.185

Graphical Abstract
  • environment and their ability to be biologically active across different species. Keywords: Leishmania; lipopeptides; molecular networking; sequence tagging; trypanosomes; Introduction Microbes belonging to the genus Bacillus are mainly Gram-positive with only a few examples characterized as Gram-negative
  • , since it promotes the ability of these ubiquitous cyclic lipopeptides to be effective and biologically active across different organism types. Hence, cyclic lipopeptides have been previously reported to possess antimicrobial, antifungal, antiviral, anticancer, and cytotoxic biological activities, but
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Published 28 Dec 2022

Redox-active molecules as organocatalysts for selective oxidative transformations – an unperceived organocatalysis field

  • Elena R. Lopat’eva,
  • Igor B. Krylov,
  • Dmitry A. Lapshin and
  • Alexander O. Terent’ev

Beilstein J. Org. Chem. 2022, 18, 1672–1695, doi:10.3762/bjoc.18.179

Graphical Abstract
  • proceeds with the preservation of stereocenters. It is tolerant to a wide range of functional groups, which makes it compatible with natural substances and complex biologically active compounds. TEMPO and its derivatives are successfully used as electrocatalysts. 4-Acetamido-2,2,6,6-tetramethylpiperidin-1
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Published 09 Dec 2022

A novel bis-triazole scaffold accessed via two tandem [3 + 2] cycloaddition events including an uncatalyzed, room temperature azide–alkyne click reaction

  • Ksenia Malkova,
  • Andrey Bubyrev,
  • Vasilisa Krivovicheva,
  • Dmitry Dar’in,
  • Alexander Bunev and
  • Mikhail Krasavin

Beilstein J. Org. Chem. 2022, 18, 1636–1641, doi:10.3762/bjoc.18.175

Graphical Abstract
  • -tetrahydro-4H-[1,2,3]triazolo[1,5-d][1,4]diazepine (A) and 5,6,7,8-tetrahydro-4H-[1,2,3]triazolo[1,5-a][1,4]diazepine (B) scaffolds are of high medicinal importance, as evident from the literature. The range of biologically active compounds based on these two closely related scaffolds (both incorporated as
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Published 02 Dec 2022

Using UHPLC–MS profiling for the discovery of new sponge-derived metabolites and anthelmintic screening of the NatureBank bromotyrosine library

  • Sasha Hayes,
  • Aya C. Taki,
  • Kah Yean Lum,
  • Joseph J. Byrne,
  • Merrick G. Ekins,
  • Robin B. Gasser and
  • Rohan A. Davis

Beilstein J. Org. Chem. 2022, 18, 1544–1552, doi:10.3762/bjoc.18.164

Graphical Abstract
  • natural product chemists have shifted their attention to marine-derived microorganisms such as bacteria and fungi over the past 10 years [2], sponges continue to be a source of novel and biologically active metabolites and remain an important taxonomic phylum for the discovery of new and bioactive natural
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Published 15 Nov 2022

Efficient synthesis of aziridinecyclooctanediol and 3-aminocyclooctanetriol

  • Emine Salamci and
  • Ayse Kilic Lafzi

Beilstein J. Org. Chem. 2022, 18, 1539–1543, doi:10.3762/bjoc.18.163

Graphical Abstract
  • and they are important building blocks in the synthesis as well as substructures of a number of biologically active natural and unnatural products [1][2][3][4][5][6][7][8]. Aziridines are valuable synthetic intermediates for the preparation of structurally complex molecules because of their
  • aziridine-fused derivatives. Some biologically active aziridine-bearing compounds 1, 2 and aminocyclitol 3. Synthesis of dimesylate 8. Synthesis of aminocyclooctanetriol 13. Synthesis of aziridinecyclooctanediol 16. Supporting Information Supporting Information File 344: Experimental section, 1H and 13C
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Published 11 Nov 2022

A facile approach to spiro[dihydrofuran-2,3'-oxindoles] via formal [4 + 1] annulation reaction of fused 1H-pyrrole-2,3-diones with diazooxindoles

  • Pavel A. Topanov,
  • Anna A. Maslivets,
  • Maksim V. Dmitriev,
  • Irina V. Mashevskaya,
  • Yurii V. Shklyaev and
  • Andrey N. Maslivets

Beilstein J. Org. Chem. 2022, 18, 1532–1538, doi:10.3762/bjoc.18.162

Graphical Abstract
  • first example of a catalyst-free formal [4 + 1] cycloaddition reaction of enones and complex diazo compounds. The synthesized compounds 3 have a pharmaceutically interesting fungal metabolites-like structure with a spiro[dihydrofuran-2,3'-oxindole] moiety. Selected examples of biologically active
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Published 10 Nov 2022

One-pot synthesis of 2-arylated and 2-alkylated benzoxazoles and benzimidazoles based on triphenylbismuth dichloride-promoted desulfurization of thioamides

  • Arisu Koyanagi,
  • Yuki Murata,
  • Shiori Hayakawa,
  • Mio Matsumura and
  • Shuji Yasuike

Beilstein J. Org. Chem. 2022, 18, 1479–1487, doi:10.3762/bjoc.18.155

Graphical Abstract
  • benzazole derivatives is of interest as they are biologically active substances. Herein, a simple method for the synthesis of 2-aryl- and 2-alkyl-substituted benzazoles is described. The reaction of 2-aminophenols with thioamides at 60 °C in the presence of triphenylbismuth dichloride in 1,2-dichloroethane
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Published 18 Oct 2022

On drug discovery against infectious diseases and academic medicinal chemistry contributions

  • Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141

Graphical Abstract
  • for simplified analogues, hopefully retaining the function of the biologically active compound, is very relevant when considering its potential in medicinal chemistry [279][280][281]. Start from leads obtained from previous research A second research direction for chemists is to start from previously
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Published 29 Sep 2022

Derivatives of benzo-1,4-thiazine-3-carboxylic acid and the corresponding amino acid conjugates

  • Péter Kisszékelyi,
  • Tibor Peňaška,
  • Klára Stankovianska,
  • Mária Mečiarová and
  • Radovan Šebesta

Beilstein J. Org. Chem. 2022, 18, 1195–1202, doi:10.3762/bjoc.18.124

Graphical Abstract
  • protease inhibitors. Given the potential usefulness of the benzothiazine scaffold as a biologically active unit and the peptidomimetic nature of many SARS-CoV-2 protease inhibitors [35], we decided to investigate the viability of attaching a 4H-benzo[b][1,4]thiazine-3-carboxylic core to amino acids
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Published 09 Sep 2022

Experimental and theoretical studies on the synthesis of 1,4,5-trisubstituted pyrrolidine-2,3-diones

  • Nguyen Tran Nguyen,
  • Vo Viet Dai,
  • Nguyen Ngoc Tri,
  • Luc Van Meervelt,
  • Nguyen Tien Trung and
  • Wim Dehaen

Beilstein J. Org. Chem. 2022, 18, 1140–1153, doi:10.3762/bjoc.18.118

Graphical Abstract
  • to obtain structurally complicated and biologically active products containing substantial portions of all starting materials [27]. Recently, polysubstituted 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones have been synthesized via eco-friendly multicomponent reactions of aromatic aldehydes, amines, and
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Published 31 Aug 2022

Electrochemical formal homocoupling of sec-alcohols

  • Kosuke Yamamoto,
  • Kazuhisa Arita,
  • Masashi Shiota,
  • Masami Kuriyama and
  • Osamu Onomura

Beilstein J. Org. Chem. 2022, 18, 1062–1069, doi:10.3762/bjoc.18.108

Graphical Abstract
  • ]. Such scaffolds are widely utilized as versatile building blocks in the synthesis of biologically active compounds [3][4][5][6][7], chiral auxiliaries [8][9], and chiral ligands [10][11][12][13]. Traditional pinacol coupling reactions are performed with a stoichiometric or even excess amount of low
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Published 22 Aug 2022

Electrochemical Friedel–Crafts-type amidomethylation of arenes by a novel electrochemical oxidation system using a quasi-divided cell and trialkylammonium tetrafluoroborate

  • Hisanori Senboku,
  • Mizuki Hayama and
  • Hidetoshi Matsuno

Beilstein J. Org. Chem. 2022, 18, 1040–1046, doi:10.3762/bjoc.18.105

Graphical Abstract
  • in organic synthesis and sometimes appear in biologically active compounds, pharmaceuticals, agrochemicals and functional molecules, amidomethylation induced by N-acyliminium ions is a helpful and valuable protocol for direct introduction of an amide function into organic molecules. Generation of N
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Published 18 Aug 2022

Synthetic strategies for the preparation of γ-phostams: 1,2-azaphospholidine 2-oxides and 1,2-azaphospholine 2-oxides

  • Jiaxi Xu

Beilstein J. Org. Chem. 2022, 18, 889–915, doi:10.3762/bjoc.18.90

Graphical Abstract
  • stereoselective asymmetric synthetic methods to access 1,2-azaphospholidine 2-oxides and 1,2-azaphospholine 2-oxides, and their fused and spiro derivatives are in high demand and should be developed in the near future. Biologically active 1,2-azaphospholine 2-oxide derivatives. Diverse synthetic strategies for
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Published 22 Jul 2022

Synthesis of novel alkynyl imidazopyridinyl selenides: copper-catalyzed tandem selenation of selenium with 2-arylimidazo[1,2-a]pyridines and terminal alkynes

  • Mio Matsumura,
  • Kaho Tsukada,
  • Kiwa Sugimoto,
  • Yuki Murata and
  • Shuji Yasuike

Beilstein J. Org. Chem. 2022, 18, 863–871, doi:10.3762/bjoc.18.87

Graphical Abstract
  • groups in many biologically active substances and pharmaceuticals, such as zolpidem, alpidem, and GSK812397 [1][2][3]. Therefore, the development of multiple chemical modification methods, at the 3-position of the imidazo[1,2-a]pyridine skeleton, for the synthesis of 3-substituted-imidazo[1,2-a]pyridines
  • concentrated under reduced pressure. The residue was purified by column chromatography using hexane/AcOEt as eluent to give the desired products 4aa–ma. Biologically active selenides having alkynyl or imidazopyridinyl groups. (a) ORTEP drawing of 4aa and (b) its stacking structure. Proposed mechanism. Control
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Published 19 Jul 2022

Synthesis of bis-spirocyclic derivatives of 3-azabicyclo[3.1.0]hexane via cyclopropene cycloadditions to the stable azomethine ylide derived from Ruhemann's purple

  • Alexander S. Filatov,
  • Olesya V. Khoroshilova,
  • Anna G. Larina,
  • Vitali M. Boitsov and
  • Alexander V. Stepakov

Beilstein J. Org. Chem. 2022, 18, 769–780, doi:10.3762/bjoc.18.77

Graphical Abstract
  • substances. Many biologically active natural products have a spirocyclic skeleton in their structure [1][2]. In this regard, there is interest in studying heterocyclic spiro compounds for drug discovery. These compounds were found to exhibit a broad range of biological activities, including antioxidant [3
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Published 29 Jun 2022

Structural basis for endoperoxide-forming oxygenases

  • Takahiro Mori and
  • Ikuro Abe

Beilstein J. Org. Chem. 2022, 18, 707–721, doi:10.3762/bjoc.18.71

Graphical Abstract
  • that play important roles in antimalarial activity by damaging membranes, inhibiting nucleic acid and protein syntheses, and so on [8][9]. The best studied endoperoxide-containing compound is probably prostaglandin H2 (PGH2), the common precursor of biologically active prostanoids [10][11][12
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Published 21 Jun 2022

Mechanochemical halogenation of unsymmetrically substituted azobenzenes

  • Dajana Barišić,
  • Mario Pajić,
  • Ivan Halasz,
  • Darko Babić and
  • Manda Ćurić

Beilstein J. Org. Chem. 2022, 18, 680–687, doi:10.3762/bjoc.18.69

Graphical Abstract
  • -coupling reactions [9][10][11][12][13][14][15][16][17][18][19] or components of pharmaceuticals and biologically active molecules [20][21]. The synthetic aspects of both approaches in solution are well established. The need for green and sustainable chemistry [22] has led to the development and synthetic
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Published 15 Jun 2022

Direct C–H amination reactions of arenes with N-hydroxyphthalimides catalyzed by cuprous bromide

  • Dongming Zhang,
  • Bin Lv,
  • Pan Gao,
  • Xiaodong Jia and
  • Yu Yuan

Beilstein J. Org. Chem. 2022, 18, 647–652, doi:10.3762/bjoc.18.65

Graphical Abstract
  • constructing C–N bonds are in high demand in organic synthesis since nitrogen-containing organic compounds are widely used in biologically active substances [1], multifunctional materials [2][3], and metal ligands [4][5]. Among them, the synthesis of aromatic amines has been important to researchers in recent
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Published 03 Jun 2022

Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment

  • Anas J. Rasras,
  • Mohamed El-Naggar,
  • Nesreen A. Safwat and
  • Raed A. Al-Qawasmeh

Beilstein J. Org. Chem. 2022, 18, 631–638, doi:10.3762/bjoc.18.63

Graphical Abstract
  • of this library will be reported in due course. Biologically active cholic acid hybridized with different heterocyclic scaffolds. Structures of target compounds 4a–v. Synthesis of cholyl 1,3,4-oxadiazole-2-thiol 2. Synthesis of cholyl 2-(propargylthio)-1,3,4-oxadiazole 3. Synthesis of target
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Published 31 May 2022

Synthesis of piperidine and pyrrolidine derivatives by electroreductive cyclization of imine with terminal dihaloalkanes in a flow microreactor

  • Yuki Naito,
  • Naoki Shida and
  • Mahito Atobe

Beilstein J. Org. Chem. 2022, 18, 350–359, doi:10.3762/bjoc.18.39

Graphical Abstract
  • , natural products, and biologically active compounds such as pergolide, scopolamine, morphine, nicotine, hygrine, and procyclidine (Figure 1) [2][3][4]. Therefore, a considerable number of synthetic approaches to pyrrolidines and piperidines have been investigated [5][6][7][8][9][10][11][12][13
  • with THF and analyzed using HPLC. Piperidine and pyrrolidine rings in biologically active compounds. Schematic diagram of the electroreductive cyclization for the synthesis of 1,2-diphenylpiperidine (3a) in an electrochemical flow microreactor. Adapted with permission from ref. [33]. Copyright 2021
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Published 29 Mar 2022
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