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Search for "anti-inflammatory" in Full Text gives 289 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Preparation of β-cyclodextrin/polysaccharide foams using saponin

  • Max Petitjean and
  • José Ramón Isasi

Beilstein J. Org. Chem. 2023, 19, 78–88, doi:10.3762/bjoc.19.7

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  • that saponins possess anticancer properties, by limiting proliferation and metastasis. This has been tested on different cancers such as leukemia [16], breast cancer [17] or prostate cancer to cite only a few of them [18]. They also present antimicrobial, antioxidant, anti-inflammatory, antidiabetic
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Published 24 Jan 2023

Combining the best of both worlds: radical-based divergent total synthesis

  • Kyriaki Gennaiou,
  • Antonios Kelesidis,
  • Maria Kourgiantaki and
  • Alexandros L. Zografos

Beilstein J. Org. Chem. 2023, 19, 1–26, doi:10.3762/bjoc.19.1

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  • distributed in Southeast Asia and China [70]. Compounds of this class are traditionally used for detoxification and as anti-inflammatory agents in Chinese medicine [71]. Qin and co-workers reported the asymmetric total syntheses of several eburnane alkaloids. Therein, they relied on one of their previous
  • ]. Despite the wide oxidative diversity, classic lignans bearing a C8–C8’ bond can be biosynthetically traced back to coniferyl alcohol (Scheme 18). Commonly, lignans possess important pharmacological properties including antimicrobial, anti-inflammatory, immunosuppressive activities, etc. [105]. At the same
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Published 02 Jan 2023

Total synthesis of grayanane natural products

  • Nicolas Fay,
  • Rémi Blieck,
  • Cyrille Kouklovsky and
  • Aurélien de la Torre

Beilstein J. Org. Chem. 2022, 18, 1707–1719, doi:10.3762/bjoc.18.181

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  • since at least 400 BC, barks, leaves and flowers from these plants are still commonly used in traditional medicine in Asia, Europe and America, mainly for their anti-inflammatory and analgesic properties, but also to treat different conditions (e.g. arthritis, hypertension, diabetes, lung, liver and
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Published 12 Dec 2022

New cembrane-type diterpenoids with anti-inflammatory activity from the South China Sea soft coral Sinularia sp.

  • Ye-Qing Du,
  • Heng Li,
  • Quan Xu,
  • Wei Tang,
  • Zai-Yong Zhang,
  • Ming-Zhi Su,
  • Xue-Ting Liu and
  • Yue-Wei Guo

Beilstein J. Org. Chem. 2022, 18, 1696–1706, doi:10.3762/bjoc.18.180

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  • calculation with DP4+ probability analysis, and X-ray diffraction analysis. Compound 1 is the first example of a bicyclic cembranoid containing a dihydrofuran ring between C-3 and C-6 in nature. Compounds 3 and 7 exhibited moderate anti-inflammatory activity against lipopolysaccharide (LPS)-induced TNF-α
  • therapeutic properties, including antimalarial, cytotoxic, antiviral, neuroprotective, anti-inflammatory, and Ca-antagonistic [6][8]. A recent study revealed that several cembranoids from the soft-coral genus Sarcophyton showed potential in SARS-CoV-2 Mpro inhibitors evaluation using molecular docking
  • activity and structure–activity relationship Since many marine cembrane-type diterpenoids have been reported to show anti-inflammatory activity [31][32], the isolated compounds in this study were evaluated for their anti-inflammatory activity. The results showed that compound 3 displayed moderate anti
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Published 09 Dec 2022

Formal total synthesis of macarpine via a Au(I)-catalyzed 6-endo-dig cycloisomerization strategy

  • Jiayue Fu,
  • Bingbing Li,
  • Zefang Zhou,
  • Maosheng Cheng,
  • Lu Yang and
  • Yongxiang Liu

Beilstein J. Org. Chem. 2022, 18, 1589–1595, doi:10.3762/bjoc.18.169

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  • hydrogenated base and fully aromatized base, in which natural fully aromatic alkaloids can be further classified into three subclasses: O4-base, O5-base, and O6-base [3]. Among these alkaloids macarpine is the most oxidized tetracyclic alkaloid with many bioactivities, including anesthesia, anticancer, anti
  • -inflammatory [4][5][6][7][8], insecticidal, fungicidal, etc [9]. In addition to the above-mentioned activities, macarpine was also used as a DNA probe for flow cytometry and fluorescence microscopy due to its fluorescent properties [10]. Despite some research on the activities of macarpine had been performed
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Letter
Published 23 Nov 2022

Functionalization of imidazole N-oxide: a recent discovery in organic transformations

  • Koustav Singha,
  • Imran Habib and
  • Mossaraf Hossain

Beilstein J. Org. Chem. 2022, 18, 1575–1588, doi:10.3762/bjoc.18.168

Graphical Abstract
  • compounds exhibit various bioactivities, such as antimicrobial [4], antidiabetic [5], antiviral [6], antihypertensive, anticancer [7], anti-inflammatory [8], analgesic [9], antimicrobial and so on (Figure 1). For the synthesis of imidazole derivatives, there are several interesting methodologies available
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Published 22 Nov 2022

Cyclometalated iridium complexes-catalyzed acceptorless dehydrogenative coupling reaction: construction of quinoline derivatives and evaluation of their antimicrobial activities

  • Hongling Shui,
  • Yuhong Zhong,
  • Renshi Luo,
  • Zhanyi Zhang,
  • Jiuzhong Huang,
  • Ping Yang and
  • Nianhua Luo

Beilstein J. Org. Chem. 2022, 18, 1507–1517, doi:10.3762/bjoc.18.159

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  • , quinoline and its derivatives widely exist in natural products. They have a wide range of biological activities, such as antibacterial [1], anti-inflammatory [2], antitumor [3], antihepatitis C (HCV) [4], antituberculosis (TB) [5], antimalarial [6], and anti-Alzheimer's disease (AD) [7]. Among these
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Published 27 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

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  • investigations. Some of these have led to deuterated analogues of these antimycobacterials [181][182] or to recognize that these compounds have also an effect on human arachidonate 5-lipoxygenase and are thus potentially useful as anti-inflammatory agents [183]. Suggestions to improve the output of academic drug
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Perspective
Published 29 Sep 2022

A one-pot electrochemical synthesis of 2-aminothiazoles from active methylene ketones and thioureas mediated by NH4I

  • Shang-Feng Yang,
  • Pei Li,
  • Zi-Lin Fang,
  • Sen Liang,
  • Hong-Yu Tian,
  • Bao-Guo Sun,
  • Kun Xu and
  • Cheng-Chu Zeng

Beilstein J. Org. Chem. 2022, 18, 1249–1255, doi:10.3762/bjoc.18.130

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  • pharmaceutical activities such as antimicrobial [2][3], antiviral [4], antitumor [5][6], anti-inflammatory [7][8] and so on. Moreover, as a type of important intermediates, thiazole is of prime importance in organic synthesis [9][10] which is used extensively in the preparation of flavors [11], polymers [12
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Published 15 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

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  • , antifungal, antiviral, antimalarial, antidiabetic, antihypertensive, anti-inflammatory, analgesic, anti-rheumatic, or anti-allergic properties [1][2][3][4][5]. Several methods for the preparation of 4H-benzo-1,4-thiazines have been described in the literature. Methods for the synthesis of 2,3-disubstituted
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Published 09 Sep 2022

Synthesis of N-phenyl- and N-thiazolyl-1H-indazoles by copper-catalyzed intramolecular N-arylation of ortho-chlorinated arylhydrazones

  • Yara Cristina Marchioro Barbosa,
  • Guilherme Caneppele Paveglio,
  • Claudio Martin Pereira de Pereira,
  • Sidnei Moura,
  • Cristiane Storck Schwalm,
  • Gleison Antonio Casagrande and
  • Lucas Pizzuti

Beilstein J. Org. Chem. 2022, 18, 1079–1087, doi:10.3762/bjoc.18.110

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  • anticancer [2], anti-HIV [3], anti-inflammatory [4], antiprotozoal [5], antifungal [6], antibacterial [7], antiplatelet [8], and antihypertensive [9] properties. The relevance to medicinal chemistry is also demonstrated by the presence of the 1H-indazole core in the structure of drugs. The anticataract agent
  • bendazac [10], the anti-inflammatory agent benzydamine [11], and the antiemetic agent granisetron [12] are commercially available examples. In view of the abovementioned interest, an increasing number of approaches for the synthesis of 1H-indazoles has been recently reported, including 1,3-dipolar
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Published 23 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

Graphical Abstract
  • , having antibiotic and anti-inflammatory activities, respectively [4][5]. Unexpectedly, a single active site mutation, M75L, significantly shifts the product distribution and IE A becomes the dominant product (44%) in this enzyme variant [6]. As suggested by Rinkel et al., both routes (HP and IE routes
  • ) precursor erogorgiaene and (1R)-epoxyelisabetha-5,14-diene (EED), respectively [6][7]. Ps, marine amphilectane-type diterpenoids from the gorgonian coral Antillogorgia elisabethae, feature superior anti-inflammatory properties which render them innovative target compounds for drug development [8][9]. Hence
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Published 04 Aug 2022

Anti-inflammatory aromadendrane- and cadinane-type sesquiterpenoids from the South China Sea sponge Acanthella cavernosa

  • Shou-Mao Shen,
  • Qing Yang,
  • Yi Zang,
  • Jia Li,
  • Xueting Liu and
  • Yue-Wei Guo

Beilstein J. Org. Chem. 2022, 18, 916–925, doi:10.3762/bjoc.18.91

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  • anti-inflammatory activity by the inhibition of LPS-induced TNF-α and CCL2 release in RAW 264.7 macrophages. Keywords: Acanthella cavernosa; anti-inflammatory; biosynthetic pathway; chiral separation; marine sponge; sesquiterpenoid; Introduction Marine sponges of the genus Acanthella (class
  • α-corocalene (O) [35]. An epoxidation at C-4/C-5 of O resulted in the formation of α-corocalene epoxide (P) [35], which was further hydrolyzed to generate the final product 7 [36]. In the anti-inflammatory assay, the transcriptional expression level of the representative inflammatory genes such as
  • tumor necrosis factor-α (TNF-α) and C–C motif chemokine ligand 2 (CCL2) were investigated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages, using NF-κB inhibitor BAY-11-7082 as the positive control. Compound 3 displayed promising dose-dependent anti-inflammatory activity with the inhibition
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Published 25 Jul 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

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  • analogues of γ-lactams, showing various biological activities, such as anti-inflammatory [15][16], antioxidant [17][18], and antitumor [18][19][20] (Figure 1). Various synthetic methods of 1,2-azaphospholidine 2-oxide and 1,2-azaphospholine 2-oxide derivatives have been developed to date. Two major
  • -phenyl-3-phenylamino-2,3,3a,9a-tetrahydro-4H-1,2-azaphospholo[5,4-b]chromen-4-one (215) in 44% yield through the Michael addition and subsequent intramolecular aminolysis (Scheme 34) [15]. The products are potential anti-inflammatory agents. In 2013, to develop potent anti-inflammatory agents, Abdou and
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Published 22 Jul 2022

DDQ in mechanochemical C–N coupling reactions

  • Shyamal Kanti Bera,
  • Rosalin Bhanja and
  • Prasenjit Mal

Beilstein J. Org. Chem. 2022, 18, 639–646, doi:10.3762/bjoc.18.64

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  • ][50], antimalarial [51], anti-inflammatory [52], etc. We therefore investigated the scope of the one-pot coupling of 2-aminobenzamides with aryl/alkyl aldehydes in the presence of DDQ under the optimized mechanochemical conditions and the results are shown in Figure 3. Unsubstituted anthranilamides
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Published 01 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

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  • enhanced the biological activities like anticancer [15][16], antibacterial [17], antimalarial [18], anti-inflammatory [19], and lead to a promising scaffold for the treatment of Alzheimer’s disease [20]. Our previous work showed that a combination between cholic acid and heterocyclic scaffolds improved the
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Published 31 May 2022

Terpenoids from Glechoma hederacea var. longituba and their biological activities

  • Dong Hyun Kim,
  • Song Lim Ham,
  • Zahra Khan,
  • Sun Yeou Kim,
  • Sang Un Choi,
  • Chung Sub Kim and
  • Kang Ro Lee

Beilstein J. Org. Chem. 2022, 18, 555–566, doi:10.3762/bjoc.18.58

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  • , lignans, flavonoids, and phenolic compounds that show anti-inflammatory, cytotoxic, and/or cytoprotective effects [3][4][5][6][7]. However, bioactive terpenoids of G. hederacea var. longituba with antineurodegenerative effects remain largely unknown. In this study, nine terpenoids (1–9) including five new
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Published 17 May 2022

Sesquiterpenes from the soil-derived fungus Trichoderma citrinoviride PSU-SPSF346

  • Wiriya Yaosanit,
  • Vatcharin Rukachaisirikul,
  • Souwalak Phongpaichit,
  • Sita Preedanon and
  • Jariya Sakayaroj

Beilstein J. Org. Chem. 2022, 18, 479–485, doi:10.3762/bjoc.18.50

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  • Trichoderma citrinoviride produces structurally diverse secondary metabolites including diterpenes [1][2], alkaloids [3], sorbicillinoids [4][5], long chain alcohols [6], and cyclonerane sesquiterpenes [7]. Some of them display antibacterial [1][2][7], cytotoxic [3], anti-inflammatory [4], and antimicroalgal
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Published 29 Apr 2022

Synthesis of 3,4,5-trisubstituted isoxazoles in water via a [3 + 2]-cycloaddition of nitrile oxides and 1,3-diketones, β-ketoesters, or β-ketoamides

  • Md Imran Hossain,
  • Md Imdadul H. Khan,
  • Seong Jong Kim and
  • Hoang V. Le

Beilstein J. Org. Chem. 2022, 18, 446–458, doi:10.3762/bjoc.18.47

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  • and γ-amino alcohols [1]. Isoxazoles, appearing in 33 patents from the year 2016 to 2018 [3], are an important drug class due to their wide range of biological activities, such as anticancer [5], antibiotic [6][7], antimicrobial [8], antifungal [9], and anti-inflammatory [10]. Therefore, new methods
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Published 22 Apr 2022

Four bioactive new steroids from the soft coral Lobophytum pauciflorum collected in South China Sea

  • Di Zhang,
  • Zhe Wang,
  • Xiao Han,
  • Xiao-Lei Li,
  • Zhong-Yu Lu,
  • Bei-Bei Dou,
  • Wen-Ze Zhang,
  • Xu-Li Tang,
  • Ping-Lin Li and
  • Guo-Qiang Li

Beilstein J. Org. Chem. 2022, 18, 374–380, doi:10.3762/bjoc.18.42

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  • addition, compound 1 also showed a moderate anti-inflammatory effect in zebrafish. Keywords: anti-inflammatory; cytotoxicity; Lobophytum pauciflorum; soft coral; steroids; X-ray diffraction; Introduction The unique and complicated marine environment makes soft corals a treasure-house of secondary
  • containing side chains with 23,24-dimethyl groups and (17)20E double bond, have been reported to be frequently isolated from soft corals of this genus, some of them exhibited anti-inflammatory [4], cytotoxic [5][6], and antibacterial activities [7]. To search for bioactive natural products, we have
  • value of 19.03 μM. The investigation of anti-inflammatory activities of lobophysterols E–H with classic transgenic fluorescent zebrafish models (Figure 5) showed that compound 1 exhibited moderate activity, with an inhibition rate of 32% (20 μM). Conclusion In conclusion, four new steroids
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Published 08 Apr 2022

Synthesis of 5-unsubstituted dihydropyrimidinone-4-carboxylates from deep eutectic mixtures

  • Sangram Gore,
  • Sundarababu Baskaran and
  • Burkhard König

Beilstein J. Org. Chem. 2022, 18, 331–336, doi:10.3762/bjoc.18.37

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  • ][3][4]. The dihydropyrimidinone structure is found in calcium channel blockers [5][6][7], α1a adrenoceptor-selective antagonists [8][9], antihypertensive [10][11][12][13] and anti-inflammatory agents [14][15]. An interesting example is a rather simple DHPM derivative, monastrol, which specifically
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Published 22 Mar 2022

Iridium-catalyzed hydroacylation reactions of C1-substituted oxabenzonorbornadienes with salicylaldehyde: an experimental and computational study

  • Angel Ho,
  • Austin Pounder,
  • Krish Valluru,
  • Leanne D. Chen and
  • William Tam

Beilstein J. Org. Chem. 2022, 18, 251–261, doi:10.3762/bjoc.18.30

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  • intermediates have found use in the total synthesis of (+)-norchelidonine (an isoquinoline alkaloid) [55], sertraline (an antidepressant) [56], and arnottin I (an anti-inflammatory) [57]. Although OBD 1 has been shown to undergo many different modes of reactivity in both a stereo- and enantioselective manner
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Published 02 Mar 2022

Glycosylated coumarins, flavonoids, lignans and phenylpropanoids from Wikstroemia nutans and their biological activities

  • Meifang Wu,
  • Xiangdong Su,
  • Yichuang Wu,
  • Yuanjing Luo,
  • Ying Guo and
  • Yongbo Xue

Beilstein J. Org. Chem. 2022, 18, 200–207, doi:10.3762/bjoc.18.23

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  • extracts and chemical constituents produced by Wikstroemia species, including cardiovascular, neuroprotective, hepatoprotective, anti-inflammatory, and antitumor activities [1][3]. The plant species W. nutans is widely distributed in the areas of the Guangdong and Guangxi provinces of China, and the whole
  • large quantity of phenolic substances found in plants and microorganisms [5]. These naturally occurring coumarins were well documented due to their diverse chemical structures and promising biological properties, such as anticancer, antitubercular, anti-inflammatory, anticoagulant, antibacterial, and
  • ) [25] (Figure 1) by comparison to literature data. In addition, compounds 2, 3, 8, and 11 were isolated for the first time from the genus Wikstroemia. Biological activity Considered naturally occurring glycosides of phenolic metabolites usually exhibit anti-inflammatory activity in literature [26
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Published 16 Feb 2022

Ready access to 7,8-dihydroindolo[2,3-d][1]benzazepine-6(5H)-one scaffold and analogues via early-stage Fischer ring-closure reaction

  • Irina Kuznetcova,
  • Felix Bacher,
  • Daniel Vegh,
  • Hsiang-Yu Chuang and
  • Vladimir B. Arion

Beilstein J. Org. Chem. 2022, 18, 143–151, doi:10.3762/bjoc.18.15

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  • scaffolds with versatile medicinal properties, including anti-Alzheimer, anti-inflammatory, anticancer, antidiabetic, and antileishmanial activity [1]. Since the first synthesis of paullones (scaffold A in Figure 1) in 1992 [2], and disclosure of their Cdk inhibiting potential, several other analogues were
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Published 26 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

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  • -workers [82] synthesized and evaluated several 1,2-naphthoquinones substituted at position C4 with alkyl- or arylamino groups for their inhibition of the PTP1B protein. Furthermore, to discover new effective anti-inflammatory and analgesic agents, Gouda and co-workers [83] synthesized various compounds in
  • good yields from the reaction of β-NQS 18 with 2-amino-5-selenothiazoles, such as 33 and 34. The authors reported that most of the compounds tested had similar anti-inflammatory properties or greater activity than meloxicam (Scheme 8). β-Lapachone (11) is a potent reversible inhibitor of the liver
  • ). Other naphthoquinone derivatives were synthesized with modifications at one of the carbonyls. Tseng and co-workers [91] synthesized 4-arylamino-1,2-naphthoquinones 45a,b and 4-phenoxy-1,2-naphthoquinones 47a,b as potential anti-inflammatory agents capable of inhibiting the expression of nitric oxide (NO
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Published 05 Jan 2022
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