Thiazolidinones: novel insights from microwave synthesis, computational studies, and potentially bioactive hybrids

• Luan A. Martinho,
• Victor H. J. G. Praciano,
• Guilherme D. R. Matos,
• Claudia C. Gatto and
• Carlos Kleber Z. Andrade

Beilstein J. Org. Chem. 2025, 21, 2618–2636, doi:10.3762/bjoc.21.203

• , ciglitazone, and rosiglitazone [9][10]. Rhodanine (2-thioxothiazolidin-4-one) derivatives exhibit a wide range of pharmacological activities, including antiviral [11], antimalarial [12], antimicrobial [13], anti-inflammatory [14], anticancer [15], antidiabetic [16], antibacterial [17], and antifungal [18

Pentacyclic aromatic heterocycles from Pd-catalyzed annulation of 1,5-diaryl-1,2,3-triazoles

• Kaylen D. Lathrum,
• Emily M. Hanneken,
• Katelyn R. Grzelak and
• James T. Fletcher

Beilstein J. Org. Chem. 2025, 21, 2524–2534, doi:10.3762/bjoc.21.194

• ][21], and materials [22][23][24]. Numerous examples of 1,4-diaryl-1,2,3-triazoles with quinoline and isoquinoline subunits have been reported, including those with anticancer [25][26][27][28][29], antiviral [30][31], antibacterial [32], antifungal [33], antimalarial [34][35], antitubercular [36], and

Assembly strategy for thieno[3,2-b]thiophenes via a disulfide intermediate derived from 3-nitrothiophene-2,5-dicarboxylate

• Roman A. Irgashev

Beilstein J. Org. Chem. 2025, 21, 2489–2497, doi:10.3762/bjoc.21.191

• attracted increasing interest as numerous TT-based compounds were proposed as promising candidates in medicinal chemistry due to their diverse pharmacological profiles including antitumor, antiviral, antimicrobial, enzymatic and phototherapeutic activities [15]. Among them, TT-2-carboxanilides exhibit

Transformation of the cyclohexane ring to the cyclopentane fragment of biologically active compounds

• Natalya Akhmetdinova,
• Ilgiz Biktagirov and
• Liliya Kh. Faizullina

Beilstein J. Org. Chem. 2025, 21, 2416–2446, doi:10.3762/bjoc.21.185

• their high potential for biological activity, such as anti-inflammatory, antimicrobial, immunomodulatory, neuroprotective, hepatoprotective, hypoglycemic, hypolipidemic, antioxidant, antispasmodic, antitumoral, antiviral, and antiallergic. The breadth of the biological action of these cyclopentanoids is

• contraction through aza-benzilic acid-type rearrangement (Scheme 13). Hasubanan-type alkaloids exhibit a wide range of biological activities, including antiviral, antimicrobial, and cytotoxic activities [46], while the biological activities and synthesis of structurally attractive norhasubanan-type alkaloids

• ], the mechanism and factors controlling the selectivity of the oxidative ring contraction in cyclic α-formyl ketones under the action of H2O2 were studied in detail. Due to their complex architecture and diverse biological activities, including antiviral, antitumor, antimalarial, and antifungal activity

Halogenated butyrolactones from the biomass-derived synthon levoglucosenone

• Johannes Puschnig,
• Martyn Jevric and
• Ben W. Greatrex

Beilstein J. Org. Chem. 2025, 21, 2297–2301, doi:10.3762/bjoc.21.175

• sofosbuvir (2). Fluorination at C2 in the nucleoside results in metabolic stability and resistance to hydrolysis as it destabilizes the formation of a C1 oxocarbenium ion [5][6]. Trifluoromethylated γ-butyrolactones also find applications as antiviral agents, for example, lactone 4 which has activity against

Discovery of cytotoxic indolo[1,2-c]quinazoline derivatives through scaffold-based design

• Daniil V. Khabarov,
• Valeria A. Litvinova,
• Lyubov G. Dezhenkova,
• Dmitry N. Kaluzhny,
• Alexander S. Tikhomirov and
• Andrey E. Shchekotikhin

Beilstein J. Org. Chem. 2025, 21, 2062–2071, doi:10.3762/bjoc.21.161

• Street, Moscow 11991, Russia 10.3762/bjoc.21.161 Abstract Indolo[1,2-c]quinazoline derivatives have emerged as promising chemotype in drug discovery due to their versatile biological activities, including antimicrobial and antiviral properties. In this study, we report the design, synthesis, and

• diverse therapeutic areas, including oncology (gefitinib, erlotinib), antiviral therapy (delavirdine, umifenovirum), CNS disorders (sertindole), and other directions (tadalafil) [4][5]. The annelation of quinazoline with nitrogen-containing heterocycles at the N(3)–C(4) bond represents a strategically

• [2,1-b]quinazoline-6,12-dione) and its derivatives are particularly noteworthy as they demonstrate multiple biological activities, including antibacterial, antitumor, antifungal, antiviral, anti-inflammatory, antileishmanial, antiplasmodial, etc. [18][19]. The structurally isomeric class – pyrimido

Bioinspired total syntheses of natural products: a personal adventure

• Zhengyi Qin,
• Yuting Yang,
• Nuran Yan,
• Xinyu Liang,
• Zhiyu Zhang,
• Yaxuan Duan,
• Huilin Li and
• Xuegong She

Beilstein J. Org. Chem. 2025, 21, 2048–2061, doi:10.3762/bjoc.21.160

• ingredients of these plants, and have elucidated a huge number of lignan natural products with novel structural backbones [32][33][34][35] (Scheme 5a). Biologically, the gymnothelignans exhibit a broad-spectrum of properties such as antiviral, antifungal, and insecticidal activities. Structurally

α-Ketoglutaric acid in Ugi reactions and Ugi/aza-Wittig tandem reactions

• Vladyslav O. Honcharov,
• Yana I. Sakhno,
• Olena H. Shvets,
• Vyacheslav E. Saraev,
• Svitlana V. Shishkina,
• Tetyana V. Shcherbakova and
• Valentyn A. Chebanov

Beilstein J. Org. Chem. 2025, 21, 2021–2029, doi:10.3762/bjoc.21.157

• reactions, widely used as a green alternative for the synthesis of active pharmaceutical ingredients [7] and opens up the possibility of creating new compounds from the class of peptidomimetics [8][9][10], which often exhibit diverse biological effects [11] including antidiabetic [12], antiviral [13

Preparation of a furfural-derived enantioenriched vinyloxazoline building block and exploring its reactivity

• Madara Darzina,
• Anna Lielpetere and
• Aigars Jirgensons

Beilstein J. Org. Chem. 2025, 21, 1737–1741, doi:10.3762/bjoc.21.136

• potent gonadotropin-releasing hormone receptor antagonists with potential application as anticancer drugs [25] and as nucleoside analogs with antiviral potency [26]. According to the reaction mechanism proposed by Elliott et al., the aza-Diels–Alder reaction of vinyloxazoline S-6 with TsNCO is a step

Microwave-enhanced additive-free C–H amination of benzoxazoles catalysed by supported copper

• Andrei Paraschiv,
• Valentina Maruzzo,
• Filippo Pettazzi,
• Stefano Magliocco,
• Paolo Inaudi,
• Daria Brambilla,
• Gloria Berlier,
• Giancarlo Cravotto and
• Katia Martina

Beilstein J. Org. Chem. 2025, 21, 1462–1476, doi:10.3762/bjoc.21.108

• pharmaceutical activity and their importance within the materials sciences [1][2]. 2-Aminobenzoxazoles, in particular, are important building blocks in the development of new bioactive compounds that can be useful as therapeutic agents with antibacterial [3], antiviral, antifungal [4], anticancer [5][6][7] and

Oxetanes: formation, reactivity and total syntheses of natural products

• Peter Gabko,
• Martin Kalník and
• Maroš Bella

Beilstein J. Org. Chem. 2025, 21, 1324–1373, doi:10.3762/bjoc.21.101

Synthesis of pyrrolo[3,2-d]pyrimidine-2,4(3H)-diones by domino C–N coupling/hydroamination reactions

• Ruben Manuel Figueira de Abreu,
• Robin Tiedemann,
• Peter Ehlers and
• Peter Langer

Beilstein J. Org. Chem. 2025, 21, 1010–1017, doi:10.3762/bjoc.21.82

• batzelladine A (D), isolated from a Bahamian sponge, possesses anti-HIV and cancerostatic activities. Antiviral properties have been identified for sangivamycin (E), which was isolated from Streptomyces rimosus (Figure 1) [16][17][18][19][20][21]. Consequently, several pyrrolopyrimidines have been synthesized

Recent total synthesis of natural products leveraging a strategy of enamide cyclization

• Chun-Yu Mi,
• Jia-Yuan Zhai and
• Xiao-Ming Zhang

Beilstein J. Org. Chem. 2025, 21, 999–1009, doi:10.3762/bjoc.21.81

• antitumor, antibacterial, antiviral, and antioxidizing properties. Previous synthetic strategies for these molecules typically rely on multi-step procedures to assemble the tricyclic core. However, the direct catalytic enantioselective formation of this scaffold from a linear precursor remains underexplored

Sequential two-step, one-pot microwave-assisted Urech synthesis of 5-monosubstituted hydantoins from L-amino acids in water

• Wei-Jin Chang,
• Sook Yee Liew,
• Thomas Kurz and
• Siow-Ping Tan

Beilstein J. Org. Chem. 2025, 21, 596–600, doi:10.3762/bjoc.21.46

• Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany 10.3762/bjoc.21.46 Abstract The hydantoin scaffold is renowned for its wide-ranging biological activities, including antibacterial, antiviral, anticancer, anti-inflammatory, and anticonvulsant effects. In

• antibacterial [1], antiviral [2], anticancer [3], anti-inflammatory [4], and anticonvulsant [5]. Hydantoins were traditionally accessed from amino acids by conversion to urea derivatives followed by cyclization (Urech reaction) or from carbonyl compounds through the cyanohydrin intermediate (Bucherer–Bergs) [6

Synthesis, characterization, antimicrobial, cytotoxic and carbonic anhydrase inhibition activities of multifunctional pyrazolo-1,2-benzothiazine acetamides

• Ayesha Saeed,
• Shahana Ehsan,
• Muhammad Zia-ur-Rehman,
• Erin M. Marshall,
• Sandra Loesgen,
• Abdus Saleem,
• Simone Giovannuzzi and
• Claudiu T. Supuran

Beilstein J. Org. Chem. 2025, 21, 348–357, doi:10.3762/bjoc.21.25

• ][15], antiviral [16], antifungal [14][17], antirheumatic [18], antiparasitic [19], insecticidal [20], antituberculous [21][22][23][24], antitumor [25], antileukemic [26], antidiabetic [27], and antifertility therapeutics [28]. Some 1,2-benzothiazine derivatives have been explored in the treatment of

Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus Samsoniella aurantia

• Rita Toshe,
• Syeda J. Khalid,
• Blondelle Matio Kemkuignou,
• Esteban Charria-Girón,
• Paul Eckhardt,
• Birthe Sandargo,
• Kunlapat Nuchthien,
• J. Jennifer Luangsa-ard,
• Till Opatz,
• Hedda Schrey,
• Sherif S. Ebada and
• Marc Stadler

Beilstein J. Org. Chem. 2025, 21, 327–339, doi:10.3762/bjoc.21.23

• Metarhizium that are known as biocontrol agents against insect pests like mosquitoes and ticks in agricultural and forestry applications [5]. Secondary metabolites produced by entomopathogenic fungi have garnered attention due to their diverse biological activities, encompassing antimicrobial, antiviral, and

Dioxazolones as electrophilic amide sources in copper-catalyzed and -mediated transformations

• Seungmin Lee,
• Minsuk Kim,
• Hyewon Han and
• Jongwoo Son

Beilstein J. Org. Chem. 2025, 21, 200–216, doi:10.3762/bjoc.21.12

• secondary amines via an N-acyl nitrene intermediate [77]. Amidines, found in biologically active compounds, have been widely investigated in medicinal chemistry due to their potent antiviral, antibacterial, anticancer, and other therapeutic properties [78][79][80][81]. As shown in Scheme 4, dioxazolones

Ceratinadin G, a new psammaplysin derivative possessing a cyano group from a sponge of the genus Pseudoceratina

• Shin-ichiro Kurimoto,
• Kouta Inoue,
• Taito Ohno and
• Takaaki Kubota

Beilstein J. Org. Chem. 2024, 20, 3215–3220, doi:10.3762/bjoc.20.267

• derivatives exhibit a range of bioactivities, including antibacterial, anticancer, antimalarial, and antiviral effects. Since the discovery of the first psammaplysin derivative, psammaplysin A [4][5], these alkaloids have been recognized as challenging targets for total synthesis. The absolute configuration

Advances in radical peroxidation with hydroperoxides

• Oleg V. Bityukov,
• Pavel Yu. Serdyuchenko,
• Andrey S. Kirillov,
• Gennady I. Nikishin,
• Vera A. Vil’ and
• Alexander O. Terent’ev

Beilstein J. Org. Chem. 2024, 20, 2959–3006, doi:10.3762/bjoc.20.249

• Nobel Prize, initiated a new era in organic peroxide chemistry. A large number of synthetic antimalarial peroxides have been prepared [3][4]. Further intensive research indicated that organic peroxides have antihelmintic, antiprotozoal, fungicidal, antiviral and other activities [5]. Therefore, the

Synthesis of pyrrole-fused dibenzoxazepine/dibenzothiazepine/triazolobenzodiazepine derivatives via isocyanide-based multicomponent reactions

• Marzieh Norouzi,
• Mohammad Taghi Nazeri,
• Ahmad Shaabani and
• Behrouz Notash

Beilstein J. Org. Chem. 2024, 20, 2870–2882, doi:10.3762/bjoc.20.241

• compounds with antibiotic, antiviral, and anticancer properties that are found in many drugs and natural products [1][2][3][4][5][6]. Pyrroles' biological properties manifest when they are fused to other heterocycles [7][8][9][10][11][12]. Among them, seven-membered heterocycles of the benzodiazepine

Synthesis and antimycotic activity of new derivatives of imidazo[1,2-a]pyrimidines

• Dmitriy Yu. Vandyshev,
• Daria A. Mangusheva,
• Khidmet S. Shikhaliev,
• Kirill A. Scherbakov,
• Oleg N. Burov,
• Alexander D. Zagrebaev,
• Tatiana N. Khmelevskaya,
• Alexey S. Trenin and
• Fedor I. Zubkov

Beilstein J. Org. Chem. 2024, 20, 2806–2817, doi:10.3762/bjoc.20.236

• polysubstituted hydrogenated heterocyclic structures on their basis [25][26][27][28], including an acetanilide fragment. The introduction of this fragment into a molecule, often drugs, enhances the cytotoxic, antibacterial, and antiviral activity of the compounds, thus widening the range of their potential

Synthesis of benzo[f]quinazoline-1,3(2H,4H)-diones

• Ruben Manuel Figueira de Abreu,
• Peter Ehlers and
• Peter Langer

Beilstein J. Org. Chem. 2024, 20, 2708–2719, doi:10.3762/bjoc.20.228

• several drugs that are still important and often used. Examples include 5-fluorouracil and brivudine. 5-Fluoruracil is an important anticancer drug, while brivudine is considered to be one of the most effective antiviral drugs against the HSV-1 virus [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18

Transition-metal-free decarbonylation–oxidation of 3-arylbenzofuran-2(3H)-ones: access to 2-hydroxybenzophenones

• Bhaskar B. Dhotare,
• Seema V. Kanojia,
• Chahna K. Sakhiya,
• Amey Wadawale and
• Dibakar Goswami

Beilstein J. Org. Chem. 2024, 20, 2655–2667, doi:10.3762/bjoc.20.223

• abilities has been verified by mathematical calculations. Keywords: decarbonylation–oxidation; hydroperoxide; 2-hydroxybenzophenone; transition-metal-free; UV-protection; Introduction Benzophenone compounds are ubiquitous in nature, and show biological activities such as anti-inflammatory, antiviral, and

Synthesis, electrochemical properties, and antioxidant activity of sterically hindered catechols with 1,3,4-oxadiazole, 1,2,4-triazole, thiazole or pyridine fragments

• Daria A. Burmistrova,
• Andrey Galustyan,
• Nadezhda P. Pomortseva,
• Kristina D. Pashaeva,
• Maxim V. Arsenyev,
• Oleg P. Demidov,
• Mikhail A. Kiskin,
• Andrey I. Poddel’sky,
• Nadezhda T. Berberova and
• Ivan V. Smolyaninov

Beilstein J. Org. Chem. 2024, 20, 2378–2391, doi:10.3762/bjoc.20.202

• heterocycles are classified as privileged medicinal scaffolds being components of many drugs [13][14]. Thiazole derivatives and their reduced forms exhibit antitumor (thiazofurin, ixabepilone), antibacterial (cefotaxime, ceftaroline, cefiderocol), antifungal (isavuconazole, fosravuconazole), antiviral

• activity against the HeLa cancer cell line [22]. 1,2,4-Triazole thioglycoside derivatives have antiviral activity against influenza strains H3N2 and H5N1 [31][32]. The 1,2,4-triazole-3-thione-imidazole hybrids displayed potential antibacterial activity against E. coli, S. aureus [33]. Heterocyclic thione

Tandem diazotization/cyclization approach for the synthesis of a fused 1,2,3-triazinone-furazan/furoxan heterocyclic system

• Yuri A. Sidunets,
• Valeriya G. Melekhina and
• Leonid L. Fershtat

Beilstein J. Org. Chem. 2024, 20, 2342–2348, doi:10.3762/bjoc.20.200

• high-energy materials [8][9][10][11][12][13]. Moreover, furazan derivatives possess antiproliferative, antibacterial, antiparasitic and antiviral activity [14][15][16]. On the other hand, furoxans referred to as unique heterocyclic compounds that exhibit NO-releasing properties under physiological

• various diseases [17][18][19][20]. Therefore, due to their NO-releasing abilities, furoxan derivatives also demonstrate anticancer, antiplatelet, antiviral and antiparasitic properties [21][22][23][24][25][26][27][28][29][30][31][32]. Another valuable nitrogen heterocyclic scaffold in medicinal chemistry