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

Synthesis and reactivity of azole-based iodazinium salts

  • Thomas J. Kuczmera,
  • Annalena Dietz,
  • Andreas Boelke and
  • Boris J. Nachtsheim

Beilstein J. Org. Chem. 2023, 19, 317–324, doi:10.3762/bjoc.19.27

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  • underwent ring openings in this reaction. This reactivity demonstrates the highly stabilizing effect of N-heterocycles on hypervalent iodine species. Furthermore, the formed 2-aminobenzimidazoles reveal new access to potential bioactive compounds [46][47]. Even the formation of the free guanidine 16 via
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Published 16 Mar 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

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  • as nystatin and nalidixic acid makes it easier to isolate them from a number of soil and sediment types using the spread plate method (SPM) in our laboratory. Therefore, in our continued research on the discovery of new bioactive compounds from Ghanaian microbes, we have started to study interesting
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Published 28 Dec 2022

Inclusion complexes of the steroid hormones 17β-estradiol and progesterone with β- and γ-cyclodextrin hosts: syntheses, X-ray structures, thermal analyses and API solubility enhancements

  • Alexios I. Vicatos,
  • Zakiena Hoossen and
  • Mino R. Caira

Beilstein J. Org. Chem. 2022, 18, 1749–1762, doi:10.3762/bjoc.18.184

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  • : cyclodextrin; complexation; 17β-estradiol; progesterone; solubility; X-ray diffraction; Introduction The insolubility of active pharmaceutical ingredients (APIs) and other bioactive compounds in aqueous media and the associated challenges for effective drug delivery are well known to have beleaguered the
  • their chemical instability, adverse side effects such as gastrointestinal irritation, and unpleasant tastes and odours [1][2][3][4][5]. Here we report an investigation of the cyclodextrin (CD) inclusion of two notable bioactive compounds (Figure 1), namely the most potent human estrogen, 17β-estradiol
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Published 22 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

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  • -cytotoxic which makes them suitable for interrogation of various biological targets. (a) Previously developed three-component approach to 1,5-disubstituted 1,2,3-triazoles; (b) double cycloaddition strategy investigated in this work. Diversely bioactive compounds based on scaffolds A and B. Aromatic azido
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Published 02 Dec 2022

Solid-phase total synthesis and structural confirmation of antimicrobial longicatenamide A

  • Takumi Matsumoto,
  • Takefumi Kuranaga,
  • Yuto Taniguchi,
  • Weicheng Wang and
  • Hideaki Kakeya

Beilstein J. Org. Chem. 2022, 18, 1560–1566, doi:10.3762/bjoc.18.166

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  • longicatenamide A was confirmed. The developed solid-phase synthesis is expected to facilitate the rapid synthesis of diverse synthetic analogues. Keywords: antimicrobial; longicatenamides; peptidic natural product; solid-phase synthesis; total synthesis; Introduction Naturally occurring bioactive compounds can
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Published 18 Nov 2022

Sinensiols H–J, three new lignan derivatives from Selaginella sinensis (Desv.) Spring

  • Qinfeng Zhu,
  • Beibei Gao,
  • Qian Chen,
  • Tiantian Luo,
  • Guobo Xu and
  • Shanggao Liao

Beilstein J. Org. Chem. 2022, 18, 1410–1415, doi:10.3762/bjoc.18.146

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  • activities [9][10][11]. However, chemical constituents responsible for its efficacy in treating various inflammatory diseases are still not clear. As part of our continuing research on the bioactive compounds from this genus [12][13], the chemical constituents of the whole plant of S. sinensis were
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Published 07 Oct 2022

Synthesis of tryptophan-dehydrobutyrine diketopiperazine and biological activity of hangtaimycin and its co-metabolites

  • Houchao Xu,
  • Anne Wochele,
  • Minghe Luo,
  • Gregor Schnakenburg,
  • Yuhui Sun,
  • Heike Brötz-Oesterhelt and
  • Jeroen S. Dickschat

Beilstein J. Org. Chem. 2022, 18, 1159–1165, doi:10.3762/bjoc.18.120

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  • , Department of Microbial Bioactive Compounds, University of Tübingen, Auf der Morgenstelle 28, 72076 Tübingen, Germany Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and School of Pharmaceutical Sciences, Wuhan University, No. 185 East Lake Road, Wuhan, 430071
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Published 07 Sep 2022

Facile and diastereoselective arylation of the privileged 1,4-dihydroisoquinolin-3(2H)-one scaffold

  • Dmitry Dar’in,
  • Grigory Kantin,
  • Alexander Bunev and
  • Mikhail Krasavin

Beilstein J. Org. Chem. 2022, 18, 1070–1078, doi:10.3762/bjoc.18.109

Graphical Abstract
  • associated biological activities and relevance to the naturally occurring alkaloids [1], 1,4-dihydro-3(2H)-isoquinolones (1,4-DHIQs) undoubtedly represent a privileged scaffold [2] for drug design considering such diversely bioactive compounds documented in the literature as ligand for serotonin 5-HT1A
  • anticancer cytotoxic agents. Diverse bioactive compounds based on the privileged 1,4-DHIQ scaffold. Strategy investigated in this work. Preparation of 3(2H)-isoquinolones 11. aObtained as a 10:1 mixture of regioisomers; purified by crystallization. bEmployed in the next step without purification (not
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Published 22 Aug 2022

Understanding the competing pathways leading to hydropyrene and isoelisabethatriene

  • Shani Zev,
  • Marion Ringel,
  • Ronja Driller,
  • Bernhard Loll,
  • Thomas Brück and
  • Dan T. Major

Beilstein J. Org. Chem. 2022, 18, 972–978, doi:10.3762/bjoc.18.97

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  • main GGPP cyclization products, along with two minor compounds, namely the isoelisabethatrienes (IEs) A (13%) and B (9%), respectively. Interestingly, the elisabethatriene diterpene macrocycle and its isoforms can act as biosynthetic precursors of the bioactive compounds erogorgiaene and pseudopterosin
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Published 04 Aug 2022

Electroreductive coupling of 2-acylbenzoates with α,β-unsaturated carbonyl compounds: density functional theory study on product selectivity

  • Naoki Kise and
  • Toshihiko Sakurai

Beilstein J. Org. Chem. 2022, 18, 956–962, doi:10.3762/bjoc.18.95

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  • attracting much attention, since bioactive compounds possessing these structures are known. This method has the potential to be applied to synthesize bioactive 2-cyanonaphthalen-1-ols [8][9] and 3-substituted phthalides [12][13][14][15][16]. The reaction mechanisms of the electroreductive coupling of 1 with
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Published 02 Aug 2022

An isoxazole strategy for the synthesis of 4-oxo-1,4-dihydropyridine-3-carboxylates

  • Timur O. Zanakhov,
  • Ekaterina E. Galenko,
  • Mikhail S. Novikov and
  • Alexander F. Khlebnikov

Beilstein J. Org. Chem. 2022, 18, 738–745, doi:10.3762/bjoc.18.74

Graphical Abstract
  • represented among drugs [5][6][7][8][9][10][11][12]. Some of bioactive compounds, such as ciprofloxacin, levofloxacin, delafloxacin, and elvitegravir, contain the fragment of 4-oxo-1,4-dihydropyridine-3-carboxylic acid [6][8] and some others, ivacaftor, dolutegravir, bictegravir, aspernigrin B, and 4PYR
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Published 23 Jun 2022

Menadione: a platform and a target to valuable compounds synthesis

  • Acácio S. de Souza,
  • Ruan Carlos B. Ribeiro,
  • Dora C. S. Costa,
  • Fernanda P. Pauli,
  • David R. Pinho,
  • Matheus G. de Moraes,
  • Fernando de C. da Silva,
  • Luana da S. M. Forezi and
  • Vitor F. Ferreira

Beilstein J. Org. Chem. 2022, 18, 381–419, doi:10.3762/bjoc.18.43

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  • makes menadione a very interesting structural model for the development of new bioactive compounds. Considering the great potential of menadione, mainly in biological applications, in this review several applications involving its synthesis and its use as a versatile synthetic platform will be discussed
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Published 11 Apr 2022

Tenacibactins K–M, cytotoxic siderophores from a coral-associated gliding bacterium of the genus Tenacibaculum

  • Yasuhiro Igarashi,
  • Yiwei Ge,
  • Tao Zhou,
  • Amit Raj Sharma,
  • Enjuro Harunari,
  • Naoya Oku and
  • Agus Trianto

Beilstein J. Org. Chem. 2022, 18, 110–119, doi:10.3762/bjoc.18.12

Graphical Abstract
  • available on the secondary metabolites from this genus [17][18]. In our continuing search for bioactive compounds from underexplored marine bacteria [19][20][21], a Tenacibaculum strain, isolated from a stony coral, was found to produce three metabolites, which turned out to be new cytotoxic hydroxamate
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Published 13 Jan 2022

1,2-Naphthoquinone-4-sulfonic acid salts in organic synthesis

  • Ruan Carlos B. Ribeiro,
  • Patricia G. Ferreira,
  • Amanda de A. Borges,
  • Luana da S. M. Forezi,
  • Fernando de Carvalho da Silva and
  • Vitor F. Ferreira

Beilstein J. Org. Chem. 2022, 18, 53–69, doi:10.3762/bjoc.18.5

Graphical Abstract
  • substituted at the C4 position of β-NQS. Despite great advances in the area, there are still many opportunities for the development of new bioactive compounds of great relevance to humanity. We hope this article will serve as a source of inspiration for current and future researchers in chemical
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Published 05 Jan 2022

Selective sulfonylation and isonitrilation of para-quinone methides employing TosMIC as a source of sulfonyl group or isonitrile group

  • Chuanhua Qu,
  • Run Huang,
  • Yong Li,
  • Tong Liu,
  • Yuan Chen and
  • Guiting Song

Beilstein J. Org. Chem. 2021, 17, 2822–2831, doi:10.3762/bjoc.17.193

Graphical Abstract
  • mixture was stirred at 80 °C for 10 h and monitored by TLC. Then, the reaction mixture was concentrated under reduced pressure followed by column chromatography over silica gel using petroleum/EtOAc 10:1 to ≈5:1 as eluent to afford the desired product 4. Selected bioactive compounds. Crystal structure of
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Published 02 Dec 2021

Recent advances in the asymmetric phosphoric acid-catalyzed synthesis of axially chiral compounds

  • Alemayehu Gashaw Woldegiorgis and
  • Xufeng Lin

Beilstein J. Org. Chem. 2021, 17, 2729–2764, doi:10.3762/bjoc.17.185

Graphical Abstract
  • scaffold for a variety of natural products, bioactive compounds and pharmacological agents [79] as well as for a variety of chiral phosphine ligands [80]. As a result, the preparation of axially chiral arylpyrroles has been one of the most important areas of investigation in synthetic chemistry. In the
  • considerable attention in recent years due to their wide application in the total synthesis of axially chiral natural products, functional materials, bioactive compounds, privileged chiral ligands, and have further potential applications in asymmetric catalysis and drug discovery. Accordingly, considerable
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Published 15 Nov 2021

The ethoxycarbonyl group as both activating and protective group in N-acyl-Pictet–Spengler reactions using methoxystyrenes. A short approach to racemic 1-benzyltetrahydroisoquinoline alkaloids

  • Marco Keller,
  • Karl Sauvageot-Witzku,
  • Franz Geisslinger,
  • Nicole Urban,
  • Michael Schaefer,
  • Karin Bartel and
  • Franz Bracher

Beilstein J. Org. Chem. 2021, 17, 2716–2725, doi:10.3762/bjoc.17.183

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  • ), and identified 1-benzyl-1,2,3,4-tetrahydroisoquinolines bearing phenoxy and benzyloxy substituents (SG-005, SG-094; for structures of bioactive compounds mentioned in this text, see Figure S1 in Supporting Information File 1) on both aromatic rings as potent blockers with promising antitumor activity
  • benzylisoquinolines 2a–f, 3a-c and 4 revealed that they possess neither antiproliferative nor P-glycoprotein blocking activity. Nevertheless, the results of this investigation represent a considerable contribution to the further development of benzyltetrahydroisoquinoline-derived bioactive compounds, since the here
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Published 05 Nov 2021

Isolation and characterization of new phenolic siderophores with antimicrobial properties from Pseudomonas sp. UIAU-6B

  • Emmanuel T. Oluwabusola,
  • Olusoji O. Adebisi,
  • Fernando Reyes,
  • Kojo S. Acquah,
  • Mercedes De La Cruz,
  • Larry L. Mweetwa,
  • Joy E. Rajakulendran,
  • Digby F. Warner,
  • Deng Hai,
  • Rainer Ebel and
  • Marcel Jaspars

Beilstein J. Org. Chem. 2021, 17, 2390–2398, doi:10.3762/bjoc.17.156

Graphical Abstract
  • transporting system as a cellular entry gateway [31][32]. Thus far, a few Pseudomonas-derived siderophores including ferrocins [33], thioquinolobactin [34], and (+)-(S)-dihydroaeruginioc acid [35] have been reported as active antimicrobial agents. Our continued exploration of new bioactive compounds from
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Published 13 Sep 2021

Nomimicins B–D, new tetronate-class polyketides from a marine-derived actinomycete of the genus Actinomadura

  • Zhiwei Zhang,
  • Tao Zhou,
  • Taehui Yang,
  • Keisuke Fukaya,
  • Enjuro Harunari,
  • Shun Saito,
  • Katsuhisa Yamada,
  • Chiaki Imada,
  • Daisuke Urabe and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2021, 17, 2194–2202, doi:10.3762/bjoc.17.141

Graphical Abstract
  • cytotoxicity against P388 murine leukemia cells with IC50 values of 33 and 89 μM, respectively. Keywords: Actinomadura; nomimicin; polyketide; spirotetronate; Introduction Actinomycetes are a valuable source of bioactive compounds, accounting for approximately two thirds of all known antibiotics, and more
  • plants, and marine invertebrates [6][7][8]. In the past 20 years, our laboratory studied the actinomycetes collected from the deep sea water (DSW) of the Sea of Japan and discovered diverse classes of bioactive compounds, such as lydicamycin congeners, γ-butyrolactones, and nyuzenamides [9][10][11
  • 2 exhibited cytotoxicity against P388 murine leukemia cells with IC50 of 33 and 89 μM, respectively. Conclusion In summary, UV-based chemical screening of bioactive compounds from marine-derived actinomycetes led to the discovery of three new polyketides, nomimicins B (1), C (2), and D (3) along
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Published 27 Aug 2021

On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets

  • Renato L. Carvalho,
  • Amanda S. de Miranda,
  • Mateus P. Nunes,
  • Roberto S. Gomes,
  • Guilherme A. M. Jardim and
  • Eufrânio N. da Silva Júnior

Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126

Graphical Abstract
  • equally effective catalysts. First-row transition (3d) metals have shown to be important catalysts in this matter. This review summarizes the use of 3d metal catalysts in C–H activation processes to obtain potentially (or proved) biologically active compounds. Keywords: bioactive compounds; C–H
  • bioactive molecules. They are also known to present valuable biological activities, such as anti-HBV (1) [44], anti-HIV (2) [45], antitumor (3) [46] and even antiplasmodial activities (4) [47] (Scheme 2A). Although these studied bioactive compounds do not directly represent the structural moieties obtained
  • evidence for radical pathways involving vanadium-peroxo species [76], with a few exceptions [95]. Vanadium-based catalysts have been employed in carbon–carbon bond formation reactions, such as arene couplings, thereby proving especially useful in the synthesis of bioactive compounds, including natural
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Published 30 Jul 2021

Natural products in the predatory defence of the filamentous fungal pathogen Aspergillus fumigatus

  • Jana M. Boysen,
  • Nauman Saeed and
  • Falk Hillmann

Beilstein J. Org. Chem. 2021, 17, 1814–1827, doi:10.3762/bjoc.17.124

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  • , physiological adaptations and chemical defence mechanisms to optimize their living conditions and resist competitors, parasites and predators [3][4][5]. These bioactive compounds are often considered as secondary metabolites (SM) which are involved in communication, symbiotic interactions, pathogenicity or
  • number of known metabolites and the interest of scientists to gain access to them remains high [7][8][9]. Genes associated with these bioactive compounds are often organized in biosynthetic gene clusters (BGCs) which are physically linked, commonly regulated and often belong to a few distinct classes of
  • ecological trigger for the production and identification of new bioactive compounds in the future. Schematic overview of fungal interactions in the environment. Fungi can be found in essentially all terrestrial habitats comprising saprophytic, parasitic, symbiotic or predatory lifestyles [6]. Independent of
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Published 28 Jul 2021

Methodologies for the synthesis of quaternary carbon centers via hydroalkylation of unactivated olefins: twenty years of advances

  • Thiago S. Silva and
  • Fernando Coelho

Beilstein J. Org. Chem. 2021, 17, 1565–1590, doi:10.3762/bjoc.17.112

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  • synthesis of new bioactive compounds [1][2]. A careful view of the carbon backbone of these natural molecules reveals their high molecular complexity [3][4][5], which can be described by the presence of multiple stereogenic centers in the same molecule, a substantial fraction of sp3 hybridized carbons (Fsp3
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Published 07 Jul 2021

Synthesis of trifluoromethyl ketones by nucleophilic trifluoromethylation of esters under a fluoroform/KHMDS/triglyme system

  • Yamato Fujihira,
  • Yumeng Liang,
  • Makoto Ono,
  • Kazuki Hirano,
  • Takumi Kagawa and
  • Norio Shibata

Beilstein J. Org. Chem. 2021, 17, 431–438, doi:10.3762/bjoc.17.39

Graphical Abstract
  • examined [46]. Trifluoromethyl ketones (TFMKs) are valuable fluorine-containing synthetic targets of bioactive compounds [55][56] that behave as mimics of the tetrahedral transition-state intermediate of enzymatic hydrolysis of esters and amides by stabilizing their hydrates (Figure 1a) [57]. In fact, the
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Published 12 Feb 2021

Regioselective chemoenzymatic syntheses of ferulate conjugates as chromogenic substrates for feruloyl esterases

  • Olga Gherbovet,
  • Fernando Ferreira,
  • Apolline Clément,
  • Mélanie Ragon,
  • Julien Durand,
  • Sophie Bozonnet,
  • Michael J. O'Donohue and
  • Régis Fauré

Beilstein J. Org. Chem. 2021, 17, 325–333, doi:10.3762/bjoc.17.30

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  • preparation of bioactive compounds with potential antioxidant properties [2][3][4][5]. Operating via a two-step serine protease mechanism involving a conserved Ser-His-Asp/Glu catalytic triad [6][7], Faes catalyze the hydrolysis of ester bonds linking hydroxycinnamoyl groups to the glycosyl moieties of plant
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Published 01 Feb 2021

The preparation and properties of 1,1-difluorocyclopropane derivatives

  • Kymbat S. Adekenova,
  • Peter B. Wyatt and
  • Sergazy M. Adekenov

Beilstein J. Org. Chem. 2021, 17, 245–272, doi:10.3762/bjoc.17.25

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Published 26 Jan 2021
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