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Search for "mode of action" in Full Text gives 90 result(s) in Beilstein Journal of Organic Chemistry.

p-Pyridinyl oxime carbamates: synthesis, DNA binding, DNA photocleaving activity and theoretical photodegradation studies

  • Panagiotis S. Gritzapis,
  • Panayiotis C. Varras,
  • Nikolaos-Panagiotis Andreou,
  • Katerina R. Katsani,
  • Konstantinos Dafnopoulos,
  • George Psomas,
  • Zisis V. Peitsinis,
  • Alexandros E. Koumbis and
  • Konstantina C. Fylaktakidou

Beilstein J. Org. Chem. 2020, 16, 337–350, doi:10.3762/bjoc.16.33

Graphical Abstract
  • , Figure 5B (For the comparable results see Figure S-6.2A and B, Supporting Information File 1). The mode of action under aerobic conditions does not involve hydroxyl radicals (in fact, DMSO seems to enhance the ds nicks), Figure 5B, well 5. It is possible that excess of this solvent facilitates the
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Published 09 Mar 2020

The interaction between cucurbit[8]uril and baicalein and the effect on baicalein properties

  • Xiaodong Zhang,
  • Jun Xie,
  • Zhiling Xu,
  • Zhu Tao and
  • Qianjun Zhang

Beilstein J. Org. Chem. 2020, 16, 71–77, doi:10.3762/bjoc.16.9

Graphical Abstract
  • the host–guest interaction packing and pattern are shown in Figure 2. 1H NMR spectroscopy is usually one of the most effective methods to characterize host–guest interactions and can be used to deduce the mode of action of the cucurbit[n]uril–guest according to the chemical shift of the proton
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Published 10 Jan 2020

Pigmentosins from Gibellula sp. as antibiofilm agents and a new glycosylated asperfuran from Cordyceps javanica

  • Soleiman E. Helaly,
  • Wilawan Kuephadungphan,
  • Patima Phainuphong,
  • Mahmoud A. A. Ibrahim,
  • Kanoksri Tasanathai,
  • Suchada Mongkolsamrit,
  • Janet Jennifer Luangsa-ard,
  • Souwalak Phongpaichit,
  • Vatcharin Rukachaisirikul and
  • Marc Stadler

Beilstein J. Org. Chem. 2019, 15, 2968–2981, doi:10.3762/bjoc.15.293

Graphical Abstract
  • . Conclusively, even though the mode of action of the pigmentosins remains to be studied, they constitute promising candidates for combination therapy with existing or novel antibiotics. So far, beauverolides have been found to be potent calmodulin (CaM) inhibitors [33], antiatherosclerotic agents [34], acyl-CoA
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Published 16 Dec 2019

Terpenes

  • Jeroen S. Dickschat

Beilstein J. Org. Chem. 2019, 15, 2966–2967, doi:10.3762/bjoc.15.292

Graphical Abstract
  • elucidation, total synthesis, biosynthetic studies, bioactivity and functionalisation for mode of action studies, and other applications of terpenes, e.g. as fragrances. I thank all colleagues who have participated in this issue for their contributions and the whole Beilstein team for the professional support
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Editorial
Published 13 Dec 2019

Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

  • Leticia Monjas,
  • Peter Fodran,
  • Johanna Kollback,
  • Carlo Cassani,
  • Thomas Olsson,
  • Maja Genheden,
  • D. G. Joakim Larsson and
  • Carl-Johan Wallentin

Beilstein J. Org. Chem. 2019, 15, 1468–1474, doi:10.3762/bjoc.15.147

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  • , no further investigations related to the conserved mode of action or toxicity were performed. Conclusion We have described the synthesis and antibacterial activity of two new truncated derivatives of AbC. Previous work indicated that the three methyl groups of AbC were not required for activity [10
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Published 02 Jul 2019

An improved synthesis of adefovir and related analogues

  • David J. Jones,
  • Eileen M. O’Leary and
  • Timothy P. O’Sullivan

Beilstein J. Org. Chem. 2019, 15, 801–810, doi:10.3762/bjoc.15.77

Graphical Abstract
  • cause nephrotoxicity [7]. The mode of action of adefovir has been widely studied and involves the inhibition of viral replication by the termination of DNA synthesis [8][9][10]. Although adefovir was described in 1986 for the first time by Holý, De Clercq and co-workers, it is still actively employed in
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Published 29 Mar 2019

Synthesis and SAR of the antistaphylococcal natural product nematophin from Xenorhabdus nematophila

  • Frank Wesche,
  • Hélène Adihou,
  • Thomas A. Wichelhaus and
  • Helge B. Bode

Beilstein J. Org. Chem. 2019, 15, 535–541, doi:10.3762/bjoc.15.47

Graphical Abstract
  • nevaltophines act as prophenoloxidase activators, it is suggested that they have a specific role in the bacteria/nematode/insect symbiosis. Little or nothing is known about the mode of action of this simple amide against S. aureus. Structure–bioactivity studies revealed that the α-keto moiety and the amide
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Published 25 Feb 2019

6’-Fluoro[4.3.0]bicyclo nucleic acid: synthesis, biophysical properties and molecular dynamics simulations

  • Sibylle Frei,
  • Andrei Istrate and
  • Christian J. Leumann

Beilstein J. Org. Chem. 2018, 14, 3088–3097, doi:10.3762/bjoc.14.288

Graphical Abstract
  • use of therapeutic antisense oligonucleotides (AONs) [1][2][3][4]. These short, synthetic fragments bind through Watson–Crick base pairing to cellular RNA, thus modulating or silencing the gene expression through various mechanisms [5][6][7]. One mode of action is the recruitment of the endonuclease
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Published 20 Dec 2018

Repurposing the anticancer drug cisplatin with the aim of developing novel Pseudomonas aeruginosa infection control agents

  • Mingjun Yuan,
  • Song Lin Chua,
  • Yang Liu,
  • Daniela I. Drautz-Moses,
  • Joey Kuok Hoong Yam,
  • Thet Tun Aung,
  • Roger W. Beuerman,
  • May Margarette Santillan Salido,
  • Stephan C. Schuster,
  • Choon-Hong Tan,
  • Michael Givskov,
  • Liang Yang and
  • Thomas E. Nielsen

Beilstein J. Org. Chem. 2018, 14, 3059–3069, doi:10.3762/bjoc.14.284

Graphical Abstract
  • . aeruginosa as compared to cisplatin (Figure 1). Mode of action The growth inhibitory effects of cisplatin on both eukaryotic cells and microbial cells are attributed to the interactions of Pt(II) in cisplatin with DNA [28][29][30]. To reveal the growth arresting mechanisms and overall impact of cisplatin on
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Published 14 Dec 2018

Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections

  • Matthew B. Calvert,
  • Varsha R. Jumde and
  • Alexander Titz

Beilstein J. Org. Chem. 2018, 14, 2607–2617, doi:10.3762/bjoc.14.239

Graphical Abstract
  • to a decline in the development of new antibiotics, with very few new antibiotics addressing a novel mode of action being brought to the market over the last four decades [3]. In parallel with the decline of new antibiotics, resistance towards these widely used drugs has evolved at a high pace and
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Published 11 Oct 2018

Microwave-assisted synthesis of biologically relevant steroidal 17-exo-pyrazol-5'-ones from a norpregnene precursor by a side-chain elongation/heterocyclization sequence

  • Gergő Mótyán,
  • László Mérai,
  • Márton Attila Kiss,
  • Zsuzsanna Schelz,
  • Izabella Sinka,
  • István Zupkó and
  • Éva Frank

Beilstein J. Org. Chem. 2018, 14, 2589–2596, doi:10.3762/bjoc.14.236

Graphical Abstract
  • known to display cytotoxic effects on diverse cancer cells by inducing a disturbance in the cell cycle and promoting apoptosis without affecting normal cellular proliferation [4][5]. In these latter cases, detailed structural criteria are still not available owing to little information about the mode of
  • action of these derivatives. Amongst steroidal 17-exo-heterocycles, those containing a pyrazole heteroaromatic ring are of special relevance with respect to the above-mentioned bioactivities [6][7][8][9]. Interestingly, so far only a few examples of compounds in which a pyrazolone moiety is attached to
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Published 08 Oct 2018

Semi-synthesis and insecticidal activity of spinetoram J and its D-forosamine replacement analogues

  • Kai Zhang,
  • Jiarong Li,
  • Honglin Liu,
  • Haiyou Wang and
  • Lamusi A

Beilstein J. Org. Chem. 2018, 14, 2321–2330, doi:10.3762/bjoc.14.207

Graphical Abstract
  • codling moth (Cydia pomonella), a major pest of pome fruits, tobacco budworm, cotton and vegetable crops [8]. Like spinosad, spinetoram elicits toxicity in the pest species via a neurotoxic mode of action. Although the exact mechanism of action has yet to be characterized, it is hypothesized that the
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Published 04 Sep 2018

Applications of organocatalysed visible-light photoredox reactions for medicinal chemistry

  • Michael K. Bogdos,
  • Emmanuel Pinard and
  • John A. Murphy

Beilstein J. Org. Chem. 2018, 14, 2035–2064, doi:10.3762/bjoc.14.179

Graphical Abstract
  • in the catalytic cycle, which itself can be classed either as reductively or oxidatively quenched. Net redox neutral processes see the substrate remain at the same oxidation state overall. These transformations are generally more complex, and the additives required as well as their mode of action
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Published 03 Aug 2018

Thiocarbonyl-enabled ferrocene C–H nitrogenation by cobalt(III) catalysis: thermal and mechanochemical

  • Santhivardhana Reddy Yetra,
  • Zhigao Shen,
  • Hui Wang and
  • Lutz Ackermann

Beilstein J. Org. Chem. 2018, 14, 1546–1553, doi:10.3762/bjoc.14.131

Graphical Abstract
  • be amenable within the cobalt-catalyzed C–H amidation manifold by weak-coordination (Scheme 3). Given the versatility of the cobalt-catalyzed C–H nitrogenation, we became intrigued to delineating its mode of action. To this end, C–H amidations in the presence of isotopically labelled co-solvents led
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Published 25 Jun 2018

Cobalt-catalyzed C–H cyanations: Insights into the reaction mechanism and the role of London dispersion

  • Eric Detmar,
  • Valentin Müller,
  • Daniel Zell,
  • Lutz Ackermann and
  • Martin Breugst

Beilstein J. Org. Chem. 2018, 14, 1537–1545, doi:10.3762/bjoc.14.130

Graphical Abstract
  • of London dispersion in these transformations. Results and Discussion Analysis of the reaction mechanism To unravel the importance of London dispersion on the cobalt-catalyzed C–H cyanation of 2-phenylpyridine (1a), the underlying catalyst’s mode of action has to be fully understood. The available
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Published 25 Jun 2018

An overview of recent advances in duplex DNA recognition by small molecules

  • Sayantan Bhaduri,
  • Nihar Ranjan and
  • Dev P. Arya

Beilstein J. Org. Chem. 2018, 14, 1051–1086, doi:10.3762/bjoc.14.93

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Published 16 May 2018

Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin–GnRH-III conjugates developed for targeted drug delivery

  • Sabine Schuster,
  • Beáta Biri-Kovács,
  • Bálint Szeder,
  • Viktor Farkas,
  • László Buday,
  • Zsuzsanna Szabó,
  • Gábor Halmos and
  • Gábor Mező

Beilstein J. Org. Chem. 2018, 14, 756–771, doi:10.3762/bjoc.14.64

Graphical Abstract
  • (Dox), daunorubicin (Dau) or epirubicin are frequently used anticancer drugs. Their mode of action is based on a planar ring system which is important for intercalation into DNA [10]. In this way, anthracyclines can affect a broad range of DNA processes leading to an inhibited synthesis of
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Published 04 Apr 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
  • and pregabalin [9][10]. Later, hydrogen-bonding activation proved to be more general for obtaining Michael adducts via the addition of 1,3-dicarbonyl compounds to nitroalkenes. Chiral thioureas and squaramides, particularly those with the bifunctional mode of action, served as excellent catalysts in
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Published 05 Mar 2018

The chemistry and biology of mycolactones

  • Matthias Gehringer and
  • Karl-Heinz Altmann

Beilstein J. Org. Chem. 2017, 13, 1596–1660, doi:10.3762/bjoc.13.159

Graphical Abstract
  • discussion of more recent contributions. Furthermore, a detailed discussion of molecular targets and structure–activity relationships is provided. Keywords: Buruli ulcer; mode of action; mycolactones; structure–activity relationships; target elucidation; total synthesis; Review I. Mycolactones and Buruli
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Published 11 Aug 2017

Strategies in megasynthase engineering – fatty acid synthases (FAS) as model proteins

  • Manuel Fischer and
  • Martin Grininger

Beilstein J. Org. Chem. 2017, 13, 1204–1211, doi:10.3762/bjoc.13.119

Graphical Abstract
  • recent years, a wealth of structural data on FAS multienzyme complexes (type I) has further deepened the insight into the principles of fatty acid (FA) synthesis [13][14][15][16][17][18][19]. Molecular mechanisms of FAS/PKS mode of action Compartmentalization Compartmentalization is a phenomenon seen
  • the three iterations for product synthesis was reported (0.1 elongations per second per set of active sites) [30]. The function of ACP The molecular details underlying the ACP mode of action are currently collaboratively decoded via structural, functional and computational methods, disclosing the
  • that the ACP mode of action in PKS is similar to FAS. The role of ACP in modular PKS is, however, complicated by the additional task of delivering the acyl moieties also to the downstream module (Figure 2c). Just rudimentary information on the nature of this translocation step is available; most
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Published 21 Jun 2017

G-Protein coupled receptors: answers from simulations

  • Timothy Clark

Beilstein J. Org. Chem. 2017, 13, 1071–1078, doi:10.3762/bjoc.13.106

Graphical Abstract
  • order to obtain a complete atomistic picture of the mode of action of the GPCR. A further problem is that we need structures that correspond to the receptors in their natural surroundings as they occur and function in nature. Proteins, especially membrane-bound ones, do not necessarily crystallize in
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Published 02 Jun 2017

Cycloheximide congeners produced by Streptomyces sp. SC0581 and photoinduced interconversion between (E)- and (Z)-2,3-dehydroanhydrocycloheximides

  • Li Yang,
  • Ping Wu,
  • Jinghua Xue,
  • Huitong Tan,
  • Zheng Zhang and
  • Xiaoyi Wei

Beilstein J. Org. Chem. 2017, 13, 1039–1049, doi:10.3762/bjoc.13.103

Graphical Abstract
  • findings suggested that these cycloheximide derivatives possibly exert the antifungal and cytotoxic activities via a similar mode of action. Conclusion Three new (1–3) and three known (4–6) cycloheximide congeners were obtained from the cultures of Streptomyces sp. SC0581. The structure elucidation of the
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Published 30 May 2017

Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis

  • Darcy J. Atkinson,
  • Briar J. Naysmith,
  • Daniel P. Furkert and
  • Margaret A. Brimble

Beilstein J. Org. Chem. 2016, 12, 2325–2342, doi:10.3762/bjoc.12.226

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  • afforded macrocycle 117 in 30–35% yield. Unfortunately efforts to remove both the Cbz and CO2H moieties of 117 to afford macrocycle 109 under hydrogenation conditions were unsuccessful. Conclusion The recent interest in teixobactin has resulted from its clinically unexploited mode of action, potent
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Published 07 Nov 2016

The direct oxidative diene cyclization and related reactions in natural product synthesis

  • Juliane Adrian,
  • Leona J. Gross and
  • Christian B. W. Stark

Beilstein J. Org. Chem. 2016, 12, 2104–2123, doi:10.3762/bjoc.12.200

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  • Rollinia membranaceae by the Cortes group [100][101]. Previous studies demonstrated, that particularly adjacent bis-THF acetogenins exhibit highly potent tumor growth inhibitory activity. Detailed investigations into the mode of action revealed that acetogenins inhibit cancer cell growth through the
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Published 30 Sep 2016

Synthesis of the C8’-epimeric thymine pyranosyl amino acid core of amipurimycin

  • Pramod R. Markad,
  • Navanath Kumbhar and
  • Dilip D. Dhavale

Beilstein J. Org. Chem. 2016, 12, 1765–1771, doi:10.3762/bjoc.12.165

Graphical Abstract
  • configurations at the C6’, C2” and C3” of the cis-pentacin are still undefined. Thus, the partially unresolved structure, a potent antifungal activity, the unexplored mode of action and the limited synthetic study make amipurimycin (1) an attractive target for futher investigation. As of now, a total synthesis
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Published 05 Aug 2016
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