Search results

Search for "bioactive compounds" in Full Text gives 212 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Current understanding and biotechnological application of the bacterial diterpene synthase CotB2

  • Ronja Driller,
  • Daniel Garbe,
  • Norbert Mehlmer,
  • Monika Fuchs,
  • Keren Raz,
  • Dan Thomas Major,
  • Thomas Brück and
  • Bernhard Loll

Beilstein J. Org. Chem. 2019, 15, 2355–2368, doi:10.3762/bjoc.15.228

Graphical Abstract
  • ], density functional theory calculations [33] as well as QM/MM simulations [37]. Variants of CotB2 open the route to a novel product portfolio with altered cyclic carbon skeletons, which can be converted into bioactive compounds by chemo-enzymatic methodologies. Modification descriptions are composed
PDF
Album
Review
Published 02 Oct 2019

Isolation and biosynthesis of an unsaturated fatty acid with unusual methylation pattern from a coral-associated bacterium Microbulbifer sp.

  • Amit Raj Sharma,
  • Enjuro Harunari,
  • Tao Zhou,
  • Agus Trianto and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2019, 15, 2327–2332, doi:10.3762/bjoc.15.225

Graphical Abstract
  • . Compound 1 showed weak growth inhibition against Saccharomyces cerevisiae. Keywords: biosynthesis; fatty acid; marine bacteria; methylation; Microbulbifer; Introduction Marine microbial symbionts are currently recognized as a reservoir of new bioactive compounds [1]. The most well-studied host animal is
PDF
Album
Supp Info
Full Research Paper
Published 30 Sep 2019

Isolation of fungi using the diffusion chamber device FIND technology

  • Benjamin Libor,
  • Henrik Harms,
  • Stefan Kehraus,
  • Ekaterina Egereva,
  • Max Crüsemann and
  • Gabriele M. König

Beilstein J. Org. Chem. 2019, 15, 2191–2203, doi:10.3762/bjoc.15.216

Graphical Abstract
  • environment. Halotolerance was to date exclusively reported for members of the Cladosporium sphaerospermum complex [28]. Analysis of genes involved in secondary metabolite production suggested Cadophora malorum as a producer of bioactive compounds [29], as later confirmed by the results of Almeida et al. [30
PDF
Album
Supp Info
Full Research Paper
Published 19 Sep 2019

Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: towards the design of photoswitchable sirtuin inhibitors

  • Christoph W. Grathwol,
  • Nathalie Wössner,
  • Sören Swyter,
  • Adam C. Smith,
  • Enrico Tapavicza,
  • Robert K. Hofstetter,
  • Anja Bodtke,
  • Manfred Jung and
  • Andreas Link

Beilstein J. Org. Chem. 2019, 15, 2170–2183, doi:10.3762/bjoc.15.214

Graphical Abstract
  • . Typically, it is not clear from the beginning, if the remodelling of the bioactive compounds will lead to an active diazeno derivative or not. The so-called azologization approach, moulded by Trauner et al., features a rational strategy for the design of photoswitchable compounds from established drug
PDF
Album
Supp Info
Full Research Paper
Published 16 Sep 2019

Molecular basis for the plasticity of aromatic prenyltransferases in hapalindole biosynthesis

  • Takayoshi Awakawa and
  • Ikuro Abe

Beilstein J. Org. Chem. 2019, 15, 1545–1551, doi:10.3762/bjoc.15.157

Graphical Abstract
  • bioactive compounds, because the prenylated compounds exhibit better bioactivities due to their improved interactions with biological membranes [3]. The aromatic PTase superfamily involved in the secondary metabolism consists of the ABBA (α-β-β-α barrel)-type [4][5], the dimethylallyltryptophan synthase
  • bioactive compounds. The reactions of aromatic PTases. The reactions catalyzed by AmbP1 (A) and AmbP3 (B). The overall structure of apo-AmbP1 (A), the Mg2+-free structure (B), and the Mg2+-bound structure (C). The active site structure of AmbP1. 1 and GSPP were bound in the active site without Mg2+ (A, Mg2
PDF
Album
Review
Published 11 Jul 2019

Synthesis of pyrrolo[1,2-a]quinolines by formal 1,3-dipolar cycloaddition reactions of quinolinium salts

  • Anthony Choi,
  • Rebecca M. Morley and
  • Iain Coldham

Beilstein J. Org. Chem. 2019, 15, 1480–1484, doi:10.3762/bjoc.15.149

Graphical Abstract
  • rise to pyrrolidine rings, prevalent in a large number of natural products and bioactive compounds. Many methods have been used to prepare azomethine ylides that undergo cycloaddition with π-systems, especially electron-poor alkenes to give pyrrolidine products [1][2][3][4]. Azomethine ylides can be
PDF
Album
Supp Info
Full Research Paper
Published 03 Jul 2019

Genomics-inspired discovery of massiliachelin, an agrochelin epimer from Massilia sp. NR 4-1

  • Jan Diettrich,
  • Hirokazu Kage and
  • Markus Nett

Beilstein J. Org. Chem. 2019, 15, 1298–1303, doi:10.3762/bjoc.15.128

Graphical Abstract
  • recognition of a far greater taxonomic diversity of microbes that can produce bioactive compounds [1][2][3]. The exploration of previously neglected taxa has been demonstrated to bear significant potential for finding new natural products and is thus highly promising from a drug discovery perspective [4][5
PDF
Album
Supp Info
Full Research Paper
Published 13 Jun 2019

Synthesis of non-racemic 4-nitro-2-sulfonylbutan-1-ones via Ni(II)-catalyzed asymmetric Michael reaction of β-ketosulfones

  • Alexander N. Reznikov,
  • Anastasiya E. Sibiryakova,
  • Marat R. Baimuratov,
  • Eugene V. Golovin,
  • Victor B. Rybakov and
  • Yuri N. Klimochkin

Beilstein J. Org. Chem. 2019, 15, 1289–1297, doi:10.3762/bjoc.15.127

Graphical Abstract
  • University, Leninskie Gory, 1, 119991, Mosсow, Russian Federation 10.3762/bjoc.15.127 Abstract Functionally substituted sulfones with stereogenic centers are valuable reagents in organic synthesis and key motifs in some bioactive compounds. The asymmetric Michael addition of β-ketosulfones to conjugated
PDF
Album
Supp Info
Full Research Paper
Published 12 Jun 2019

Doebner-type pyrazolopyridine carboxylic acids in an Ugi four-component reaction

  • Maryna V. Murlykina,
  • Oleksandr V. Kolomiets,
  • Maryna M. Kornet,
  • Yana I. Sakhno,
  • Sergey M. Desenko,
  • Victoriya V. Dyakonenko,
  • Svetlana V. Shishkina,
  • Oleksandr A. Brazhko,
  • Vladimir I. Musatov,
  • Alexander V. Tsygankov,
  • Erik V. Van der Eycken and
  • Valentyn A. Chebanov

Beilstein J. Org. Chem. 2019, 15, 1281–1288, doi:10.3762/bjoc.15.126

Graphical Abstract
  • synergetic application of several diversity-oriented synthesis (DOS) instruments allows an effective decoration of the privileged scaffolds for creating collections of unique, highly potent bioactive compounds [4][5]. The pyrazolopyridine scaffold can be regarded as a privileged motif as it exhibits various
PDF
Album
Supp Info
Full Research Paper
Published 12 Jun 2019

Robust perfluorophenylboronic acid-catalyzed stereoselective synthesis of 2,3-unsaturated O-, C-, N- and S-linked glycosides

  • Madhu Babu Tatina,
  • Xia Mengxin,
  • Rao Peilin and
  • Zaher M. A. Judeh

Beilstein J. Org. Chem. 2019, 15, 1275–1280, doi:10.3762/bjoc.15.125

Graphical Abstract
  • molecular recognition, cell–cell interaction, immunological recognition and transmission of biological information [4][5][6]. They are easily transformed into important bioactive compounds such as oligosaccharides, glycopeptides, nucleosides, antibiotics, uronic acids and other natural products [1][2][3
PDF
Album
Supp Info
Full Research Paper
Published 11 Jun 2019

Efficient synthesis of pyrazolopyridines containing a chromane backbone through domino reaction

  • Razieh Navari,
  • Saeed Balalaie,
  • Saber Mehrparvar,
  • Fatemeh Darvish,
  • Frank Rominger,
  • Fatima Hamdan and
  • Sattar Mirzaie

Beilstein J. Org. Chem. 2019, 15, 874–880, doi:10.3762/bjoc.15.85

Graphical Abstract
  • tracazolate, cartazolate, and etazolate [22]. Other pyrazolopyridine-containing bioactive compounds include a GSK-3 inhibitor [23] and BAY 41-2272, [24][25] and could be used as cardiovascular therapeutic agents (Figure 1). Moreover, pyrazolopyridine derivatives also have industrial importance as fluorophores
PDF
Album
Supp Info
Full Research Paper
Published 11 Apr 2019

Catalyst-free assembly of giant tris(heteroaryl)methanes: synthesis of novel pharmacophoric triads and model sterically crowded tris(heteroaryl/aryl)methyl cation salts

  • Rodrigo Abonia,
  • Luisa F. Gutiérrez,
  • Braulio Insuasty,
  • Jairo Quiroga,
  • Kenneth K. Laali,
  • Chunqing Zhao,
  • Gabriela L. Borosky,
  • Samantha M. Horwitz and
  • Scott D. Bunge

Beilstein J. Org. Chem. 2019, 15, 642–654, doi:10.3762/bjoc.15.60

Graphical Abstract
  • ]. Furthermore, it is highly desirable to perform these reactions in environmentally friendly solvents such as water, ethanol, and PEG [6][7]. Motifs bearing triarylmethane (Ar3CH) [8][9][10] and their heterocyclic variants (Het-Ar)3CH [8][9][10][11][12], constitute an integral part of a number of bioactive
  • compounds [13][14][15][16]. Due to their valuable properties, they are also well exploited by the chemical industry as dyes and photochromic agents [17][18], protective groups in organic synthesis [19] and as building blocks for dendrimers [20] and nonlinear optical (NLO) properties [21] (Scheme 1
PDF
Album
Supp Info
Full Research Paper
Published 12 Mar 2019

Synthesis and selected transformations of 2-unsubstituted 1-(adamantyloxy)imidazole 3-oxides: straightforward access to non-symmetric 1,3-dialkoxyimidazolium salts

  • Grzegorz Mlostoń,
  • Małgorzata Celeda,
  • Katarzyna Urbaniak,
  • Marcin Jasiński,
  • Vladyslav Bakhonsky,
  • Peter R. Schreiner and
  • Heinz Heimgartner

Beilstein J. Org. Chem. 2019, 15, 497–505, doi:10.3762/bjoc.15.43

Graphical Abstract
  • , alkoxyamines are known not only as bioactive compounds [19][20] but also as important initiators of polymerization processes that have been extensively studied in the recent decade [21]. Among alkoxyamines, adamantyloxyamine (4) occupies a prominent position, and for that reason it was selected for experiments
  • alkaloids, which found wide application in some regions as food-stuff and medical supply [33]. The method described in the present study opens a straightforward access to their benzyloxy analogues, potentially bioactive compounds, which have not been known yet. Experimental General information: Solvents and
PDF
Album
Supp Info
Full Research Paper
Published 19 Feb 2019

Thiol-free chemoenzymatic synthesis of β-ketosulfides

  • Adrián A. Heredia,
  • Martín G. López-Vidal,
  • Marcela Kurina-Sanz,
  • Fabricio R. Bisogno and
  • Alicia B. Peñéñory

Beilstein J. Org. Chem. 2019, 15, 378–387, doi:10.3762/bjoc.15.34

Graphical Abstract
  • role as precursors in the synthesis of bioactive compounds [13][26][27], substrates for multicomponent reactions [28], and lately, have successfully been applied in polymer photodecoration [29][30]. They can easily be reduced into chiral hydroxy derivatives [31] and properly oxidised at sulfur to
PDF
Album
Supp Info
Full Research Paper
Published 11 Feb 2019

Sigmatropic rearrangements of cyclopropenylcarbinol derivatives. Access to diversely substituted alkylidenecyclopropanes

  • Guillaume Ernouf,
  • Jean-Louis Brayer,
  • Christophe Meyer and
  • Janine Cossy

Beilstein J. Org. Chem. 2019, 15, 333–350, doi:10.3762/bjoc.15.29

Graphical Abstract
  • alkylidenecyclopropanes are also synthetically useful [1][2][3][4][5][6]. The importance of this latter class of transformations is obviously related to the widespread occurrence of cyclopropanes in natural and/or bioactive compounds [7][8] and the great interest of the cyclopropyl core in new drugs development [9
PDF
Album
Review
Published 05 Feb 2019

Asymmetric synthesis of a high added value chiral amine using immobilized ω-transaminases

  • Antonella Petri,
  • Valeria Colonna and
  • Oreste Piccolo

Beilstein J. Org. Chem. 2019, 15, 60–66, doi:10.3762/bjoc.15.6

Graphical Abstract
  • and in particular compounds with an amino functional group such as 3-aminopiperidine are valuable intermediates for the production of a large number of bioactive compounds with pharmacological properties. In this paper, the synthesis of both enantiomers of 3-amino-1-Boc-piperidine by amination of the
PDF
Album
Full Research Paper
Published 07 Jan 2019

Molecular iodine-catalyzed one-pot multicomponent synthesis of 5-amino-4-(arylselanyl)-1H-pyrazoles

  • Camila S. Pires,
  • Daniela H. de Oliveira,
  • Maria R. B. Pontel,
  • Jean C. Kazmierczak,
  • Roberta Cargnelutti,
  • Diego Alves,
  • Raquel G. Jacob and
  • Ricardo F. Schumacher

Beilstein J. Org. Chem. 2018, 14, 2789–2798, doi:10.3762/bjoc.14.256

Graphical Abstract
  • importance in bioactive compounds, pharmaceuticals, and as chemical intermediates for organic and inorganic synthesis [1][2]. As a consequence, the development of efficient and practical methods for C–Se bond formation is still a promising field of research in organic chemistry. Despite the several number of
PDF
Album
Supp Info
Full Research Paper
Published 06 Nov 2018

Synthesis of a tyrosinase inhibitor by consecutive ethenolysis and cross-metathesis of crude cashew nutshell liquid

  • Jacqueline Pollini,
  • Valentina Bragoni and
  • Lukas J. Gooßen

Beilstein J. Org. Chem. 2018, 14, 2737–2744, doi:10.3762/bjoc.14.252

Graphical Abstract
  • ]. A limited number of derivatizations of anacardic acid are reported by now, including the synthesis of lactones [18][19][20], sulfonamides [21] or hydrazones [22], typically bioactive compounds though with low commercial value. However, several studies suggest that anacardic acid and its derivatives
PDF
Album
Supp Info
Full Research Paper
Published 31 Oct 2018

Some mechanistic aspects regarding the Suzuki–Miyaura reaction between selected ortho-substituted phenylboronic acids and 3,4,5-tribromo-2,6-dimethylpyridine

  • Piotr Pomarański,
  • Piotr Roszkowski,
  • Jan K. Maurin,
  • Armand Budzianowski and
  • Zbigniew Czarnocki

Beilstein J. Org. Chem. 2018, 14, 2384–2393, doi:10.3762/bjoc.14.214

Graphical Abstract
  • selectivity using a differently ortho-substituted phenylbornic acid was observed. Keywords: arylpyridines; atropisomerism; cross-coupling; palladium; Suzuki–Miyaura reaction; Introduction Axially chiral biaryls not only subsist in many classes of natural and bioactive compounds [1][2] but also are an
PDF
Album
Supp Info
Full Research Paper
Published 11 Sep 2018

Synthesis of 1,4-imino-L-lyxitols modified at C-5 and their evaluation as inhibitors of GH38 α-mannosidases

  • Maroš Bella,
  • Sergej Šesták,
  • Ján Moncoľ,
  • Miroslav Koóš and
  • Monika Poláková

Beilstein J. Org. Chem. 2018, 14, 2156–2162, doi:10.3762/bjoc.14.189

Graphical Abstract
  • ; inhibitors; pyrrolidines; synthesis; Introduction Carbohydrates as chiral templates for a construction of bioactive compounds are of steady interest in medicinal chemistry [1][2][3]. The polyfunctional nature of carbohydrate units offers many possibilities for the design of a wide variety of new compounds
  • . Moreover, various desired substituents can be selectively appended to any required position of the carbohydrate unit. This leads to a preparation of mimetics that meet the requirements of metabolically more stable bioactive compounds. During the years, many scaffolds based on monosaccharides [4
  • ], disaccharides or higher oligosaccharides [5][6] as well as multivalent [7][8] carbohydrate units have been developed. These glycomimetics and glycopeptides have also found applications as bioactive compounds [9][10]. One group of the scaffolds includes iminosugars [11][12] as analogues of the monosaccharides
PDF
Album
Supp Info
Full Research Paper
Published 17 Aug 2018

Rhodium-catalyzed C–H functionalization of heteroarenes using indoleBX hypervalent iodine reagents

  • Erwann Grenet,
  • Ashis Das,
  • Paola Caramenti and
  • Jérôme Waser

Beilstein J. Org. Chem. 2018, 14, 1208–1214, doi:10.3762/bjoc.14.102

Graphical Abstract
  • also omnipresent in bioactive compounds [2]. It can be directly bound to other heterocycles, such as a dihydropyrazidinone in hamacanthine A (4) (Figure 1) [3]. Due to their occurrence in biologically active compounds, it is therefore attractive to develop new methods to functionalize pyridinones. The
  • building blocks in the search for new bioactive compounds. Results and Discussion We started the studies on C–H indolation with the optimization of the reactions conditions (Table 1) for the coupling of [1,2'-bipyridin]-2-one (5a) with Me-indoleBX 6a, easily obtained from commercially available 1
  • separated and the aqueous layer was extracted twice with DCM (5 mL). The organic layers were combined, dried over magnesium sulfate dehydrate, filtered and concentrated under reduced pressure. The crude residue was purified by preparative TLC using DCM/MeOH to afford the pure desired compound. Bioactive
PDF
Album
Supp Info
Letter
Published 25 May 2018

Fluorocyclisation via I(I)/I(III) catalysis: a concise route to fluorinated oxazolines

  • Felix Scheidt,
  • Christian Thiehoff,
  • Gülay Yilmaz,
  • Stephanie Meyer,
  • Constantin G. Daniliuc,
  • Gerald Kehr and
  • Ryan Gilmour

Beilstein J. Org. Chem. 2018, 14, 1021–1027, doi:10.3762/bjoc.14.88

Graphical Abstract
  • . Selected examples of bioactive compounds containing the 2-oxazoline motif. The catalytic difluorination of alkenes (top) and the proposed fluorocyclisation via the same I(I)/I(III) manifold (bottom). Substrate scope. aReaction conducted on 1 mmol scale. bReaction time increased to 40 hours. cReaction time
PDF
Album
Supp Info
Full Research Paper
Published 09 May 2018

Investigations towards the stereoselective organocatalyzed Michael addition of dimethyl malonate to a racemic nitroalkene: possible route to the 4-methylpregabalin core structure

  • Denisa Vargová,
  • Rastislav Baran and
  • Radovan Šebesta

Beilstein J. Org. Chem. 2018, 14, 553–559, doi:10.3762/bjoc.14.42

Graphical Abstract
  • stereoselective synthesis of bioactive compounds [1][2][3]. In particular, stereoselective conversions of nitro compounds served in many syntheses of pharmaceuticals [4]. Derivatives of γ-aminobutyric acid are an important class of medicines targeting problems with the central nervous system, such as pains
PDF
Album
Supp Info
Full Research Paper
Published 05 Mar 2018

Synthesis of fluoro-functionalized diaryl-λ3-iodonium salts and their cytotoxicity against human lymphoma U937 cells

  • Prajwalita Das,
  • Etsuko Tokunaga,
  • Hidehiko Akiyama,
  • Hiroki Doi,
  • Norimichi Saito and
  • Norio Shibata

Beilstein J. Org. Chem. 2018, 14, 364–372, doi:10.3762/bjoc.14.24

Graphical Abstract
  • ]. Hypervalent iodine compounds have been receiving a lot of attention lately due to their varied applications in organic synthesis [33][34][35][36][37][38][39][40]. A wide range of bioactive compounds make use of diaryliodonium reagents as a part of their synthesis [41][42][43]. On the other hand, there are
PDF
Album
Supp Info
Full Research Paper
Published 07 Feb 2018

Nucleophilic fluoroalkylation/cyclization route to fluorinated phthalides

  • Masanori Inaba,
  • Tatsuya Sakai,
  • Shun Shinada,
  • Tsuyuka Sugiishi,
  • Yuta Nishina,
  • Norio Shibata and
  • Hideki Amii

Beilstein J. Org. Chem. 2018, 14, 182–186, doi:10.3762/bjoc.14.12

Graphical Abstract
  • synthesis of useful bioactive compounds. There is a growing interest in the usefulness of phthalides and their derivatives. Organofluorine compounds often show attractive physical, chemical, and biological properties and are widely used in many fields, such as pharmaceuticals, agrochemicals, and materials
PDF
Album
Supp Info
Full Research Paper
Published 19 Jan 2018
Other Beilstein-Institut Open Science Activities