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Search for "antiviral" in Full Text gives 290 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

15N-Labelling and structure determination of adamantylated azolo-azines in solution

  • Sergey L. Deev,
  • Alexander S. Paramonov,
  • Tatyana S. Shestakova,
  • Igor A. Khalymbadzha,
  • Oleg N. Chupakhin,
  • Julia O. Subbotina,
  • Oleg S. Eltsov,
  • Pavel A. Slepukhin,
  • Vladimir L. Rusinov,
  • Alexander S. Arseniev and
  • Zakhar O. Shenkarev

Beilstein J. Org. Chem. 2017, 13, 2535–2548, doi:10.3762/bjoc.13.250

Graphical Abstract
  • against influenza A virus compared with the currently used antiviral drug rimantadine (1-(1-adamantyl)ethanamine) [3]. More recently, Roberge et al. described new inhibitors of the influenza A virus M2 proton channel. Among the studied compounds, adamantyl imidazole 3 showed good activity [4]. An azolo
  • ][1,2,4]triazine 4 (Figure 1A, Triazavirin®) was approved in Russia for the treatment of influenza [9]. This drug targets the viral protein haemagglutinin. The incorporation of an adamantyl moiety in azolo-azine structures could lead to the development of new multifunctional antiviral drugs. Previously
  • tetrazolo[1,5-b][1,2,4]triazin-7-one in TFA solution. The formation of an adamantyl cation and NH-tetrazolo-triazine during the isomerization reaction was confirmed. (A) Adamantylated azoles and derivatives of 1,2,4-triazolo[5,1-c][1,2,4]triazine with antiviral activities. (B) Four sites sensitive to N
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Published 29 Nov 2017

Pyrene–nucleobase conjugates: synthesis, oligonucleotide binding and confocal bioimaging studies

  • Artur Jabłoński,
  • Yannic Fritz,
  • Hans-Achim Wagenknecht,
  • Rafał Czerwieniec,
  • Tytus Bernaś,
  • Damian Trzybiński,
  • Krzysztof Woźniak and
  • Konrad Kowalski

Beilstein J. Org. Chem. 2017, 13, 2521–2534, doi:10.3762/bjoc.13.249

Graphical Abstract
  • detecting markers [14], as fluorescent DNA probes [15], non-covalent binders to canonical oligonucleotide templates [16], and antiviral agents [17][18]. Notably, pyrene excimer formation in DNA template assemblies is much less efficient than in normal pyrene conjugates due to the helical twist between
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Published 28 Nov 2017

Fluorination of some highly functionalized cycloalkanes: chemoselectivity and substrate dependence

  • Attila Márió Remete,
  • Melinda Nonn,
  • Santos Fustero,
  • Matti Haukka,
  • Ferenc Fülöp and
  • Loránd Kiss

Beilstein J. Org. Chem. 2017, 13, 2364–2371, doi:10.3762/bjoc.13.233

Graphical Abstract
  • amino acids and their analogous derivatives have gained considerable interest in pharmaceutical chemistry as bioactive compounds. Some derivatives (e.g., peramivir, oseltamivir or laninamivir) are known as antiviral drugs [19][20][21][22], while other cyclopentane β-amino acids (e.g., icofungipen
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Published 06 Nov 2017

Diosgenyl 2-amino-2-deoxy-β-D-galactopyranoside: synthesis, derivatives and antimicrobial activity

  • Henryk Myszka,
  • Patrycja Sokołowska,
  • Agnieszka Cieślińska,
  • Andrzej Nowacki,
  • Maciej Jaśkiewicz,
  • Wojciech Kamysz and
  • Beata Liberek

Beilstein J. Org. Chem. 2017, 13, 2310–2315, doi:10.3762/bjoc.13.227

Graphical Abstract
  • diosgenyl saponins are used in folk medicine in many countries. Such herbal medicines exhibit anti-inflammatory, antibacterial, antifungal, antiviral, diuretic and expectorant activities [2][11]. Importantly, these also help fight cancer cells [12][13][14]. Although saponins, in which D-galactose is
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Published 01 Nov 2017

Preparation of imidazo[1,2-a]-N-heterocyclic derivatives with gem-difluorinated side chains

  • Layal Hariss,
  • Kamal Bou Hadir,
  • Mirvat El-Masri,
  • Thierry Roisnel,
  • René Grée and
  • Ali Hachem

Beilstein J. Org. Chem. 2017, 13, 2115–2121, doi:10.3762/bjoc.13.208

Graphical Abstract
  • compounds are frequently found in bioactive naturally occurring compounds, as well as in the synthetic pharmacopeia. Imidazo[1,2-a]pyridine is an important heterocyclic system present in many molecules featuring diverse biological activities, such as antiviral, antimicrobial, antitumor, anti-inflammatory
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Published 10 Oct 2017

Oxidative dehydrogenation of C–C and C–N bonds: A convenient approach to access diverse (dihydro)heteroaromatic compounds

  • Santanu Hati,
  • Ulrike Holzgrabe and
  • Subhabrata Sen

Beilstein J. Org. Chem. 2017, 13, 1670–1692, doi:10.3762/bjoc.13.162

Graphical Abstract
  • alkaloids such as luotonin A, tryptanthrin and many more (Figure 1) [11][12]. Quinazoline derivatives work as potential inhibitors of epidermal growth factor (EGF) and tyrosine kinase receptors and also display antibacterial, antitubercular and antiviral properties [13][14][15][16]. Last but not the least
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Published 15 Aug 2017

Effect of uridine protecting groups on the diastereoselectivity of uridine-derived aldehyde 5’-alkynylation

  • Raja Ben Othman,
  • Mickaël J. Fer,
  • Laurent Le Corre,
  • Sandrine Calvet-Vitale and
  • Christine Gravier-Pelletier

Beilstein J. Org. Chem. 2017, 13, 1533–1541, doi:10.3762/bjoc.13.153

Graphical Abstract
  • ; nucleoside; protecting groups; uridine; Introduction Nucleoside and nucleotide derivatives or analogues are biologically active compounds of major interest [1][2]. Their widespread applications span from therapeutic agents, such as antibacterial [3][4][5], antiviral [6] or antitumor [7][8] drugs, to
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Published 04 Aug 2017

A speedy route to sterically encumbered, benzene-fused derivatives of privileged, naturally occurring hexahydropyrrolo[1,2-b]isoquinoline

  • Olga Bakulina,
  • Alexander Ivanov,
  • Vitalii Suslonov,
  • Dmitry Dar’in and
  • Mikhail Krasavin

Beilstein J. Org. Chem. 2017, 13, 1413–1424, doi:10.3762/bjoc.13.138

Graphical Abstract
  • plethora of biological activities displayed by the lycorine and tylophorine alkaloids (such as pro-apoptotic [22], antiviral [23], hypoxia-inducible factor-1 inhibitory [24]), the scaffold can be confidently regarded as privileged [25]. Recently, we [26] and others [27] reported the use of indolenines as
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Published 18 Jul 2017

Aqueous semisynthesis of C-glycoside glycamines from agarose

  • Juliana C. Cunico Dallagnol,
  • Alexandre Orsato,
  • Diogo R. B. Ducatti,
  • Miguel D. Noseda,
  • Maria Eugênia R. Duarte and
  • Alan G. Gonçalves

Beilstein J. Org. Chem. 2017, 13, 1222–1229, doi:10.3762/bjoc.13.121

Graphical Abstract
  • employed in drug discovery. A part of our group has utilized this type of approach for the synthesis of dihydropyridine glycoconjugates [9] and antiviral sulfated alkylglycosides [10]. In an effort to amplify the utility of AnGal as a starting material for the synthesis of bioactive compounds, we have
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Published 23 Jun 2017

An eco-compatible strategy for the diversity-oriented synthesis of macrocycles exploiting carbohydrate-derived building blocks

  • Sushil K. Maurya and
  • Rohit Rana

Beilstein J. Org. Chem. 2017, 13, 1106–1118, doi:10.3762/bjoc.13.110

Graphical Abstract
  • , macrocyclic glycolipids have shown phosphatase inhibition, cytotoxicity and antiviral activities [12][14]. Generally, the synthesis of these molecules involves a multi-step construction of linear precursors incorporating synthetically compatible functional groups followed by a cyclization in the late stage of
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Published 09 Jun 2017

New tricks of well-known aminoazoles in isocyanide-based multicomponent reactions and antibacterial activity of the compounds synthesized

  • Maryna V. Murlykina,
  • Maryna N. Kornet,
  • Sergey M. Desenko,
  • Svetlana V. Shishkina,
  • Oleg V. Shishkin,
  • Aleksander A. Brazhko,
  • Vladimir I. Musatov,
  • Erik V. Van der Eycken and
  • Valentin A. Chebanov

Beilstein J. Org. Chem. 2017, 13, 1050–1063, doi:10.3762/bjoc.13.104

Graphical Abstract
  • , anti-inflammatory [28][43], antiviral [39][44], antidiabetic [45] effects and cancer cell growth-inhibitory features should be mentioned [29][46][47][48]. Ugi-4CR has been applied in the synthesis of natural products, as bicyclomycin, furanomycin, penicillin etc. [53]. The high combinatorial potential
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Published 31 May 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
  • a multitude of biological activities. The most famous representative of this family, cycloheximide (5), has been used for decades as an inhibitor of eukaryotic translation elongation [1][2][3]. Other members of this family show potent cell migration inhibition and antiviral activity [4][5][6], which
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Published 30 May 2017

Glyco-gold nanoparticles: synthesis and applications

  • Federica Compostella,
  • Olimpia Pitirollo,
  • Alessandro Silvestri and
  • Laura Polito

Beilstein J. Org. Chem. 2017, 13, 1008–1021, doi:10.3762/bjoc.13.100

Graphical Abstract
  • treatment of HIV infection. β-D-Glucose coated AuNPs have been decorated with the antiviral drugs abacavir (ABC) and lamivudine (3TC) and used as delivery systems. These co-drug structures were able to release the drugs in acidic conditions to inhibit viral replication in cellular assays [91]. GAuNPs
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Published 24 May 2017

First total synthesis of kipukasin A

  • Chuang Li,
  • Haixin Ding,
  • Zhizhong Ruan,
  • Yirong Zhou and
  • Qiang Xiao

Beilstein J. Org. Chem. 2017, 13, 855–862, doi:10.3762/bjoc.13.86

Graphical Abstract
  • number of antiviral and antitumor drugs [3][4]. On the other hand, naturally occurring nucleosides, especially marine nucleosides, have also played an indispensable role in drug discovery, which make great contribution in the commercialization of cytosine arabinoside (Ara-C), adenine arabinoside (Ara-A
  • ) and AZT, etc. [5][6]. Nucleosides and their analogues will continue to play an important role in future drug discovery [7]. In the past decades, exploration of novel naturally occurring marine nucleosides has made expeditious achievements [8][9][10]. Some of them showed promising antibiotic, antiviral
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Published 09 May 2017

Opportunities and challenges for the sustainable production of structurally complex diterpenoids in recombinant microbial systems

  • Katarina Kemper,
  • Max Hirte,
  • Markus Reinbold,
  • Monika Fuchs and
  • Thomas Brück

Beilstein J. Org. Chem. 2017, 13, 845–854, doi:10.3762/bjoc.13.85

Graphical Abstract
  • stereoselective synthesis of (1R,3E,7E,11S,12S)-3,7,18-dolabellatriene, a bicyclic diterpene (Scheme 2). Dollabellanes derive mostly from marine organisms and display bioactivities such as antiviral and cytotoxic effects [59]. Dolabellatriene from a reprogrammed CotB2 contribute with antimicrobial activity
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Published 08 May 2017

A practical and efficient approach to imidazo[1,2-a]pyridine-fused isoquinolines through the post-GBB transformation strategy

  • Taofeng Shao,
  • Zhiming Gong,
  • Tianyi Su,
  • Wei Hao and
  • Chao Che

Beilstein J. Org. Chem. 2017, 13, 817–824, doi:10.3762/bjoc.13.82

Graphical Abstract
  • (Figure 1) [6]. Furthermore, the isoquinoline motif represents a privileged medicinal skeleton widely found in a number of natural alkaloids and pharmaceutically active compounds [7]. Some of them exhibit diversified biological properties, including anti-inflammatory [8], antibacterial [9], antiviral [10
  • ], and antitumor activities [11]. For example, the natural alkaloids berberine (IV) and narciclasine (V) possess antiplasmodial and antiviral activity, respectively [12][13]. Indotecan (VI) and its analog idimitecan (VII) were identified as topoisomerase I inhibitors, and were promoted into phase I
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Published 04 May 2017

New approach toward the synthesis of deuterated pyrazolo[1,5-a]pyridines and 1,2,4-triazolo[1,5-a]pyridines

  • Aleksey Yu. Vorob’ev,
  • Vyacheslav I. Supranovich,
  • Gennady I. Borodkin and
  • Vyacheslav G. Shubin

Beilstein J. Org. Chem. 2017, 13, 800–805, doi:10.3762/bjoc.13.80

Graphical Abstract
  • antiviral [7][8], antimalarial [9] and antitubercular [10] agents. Also they were applied in the development of FIXa [11], PI3K [12], EGFR [13] and PDE [14] inhibitors and dopamine receptor ligands [15]. The nonselective PDE3,4 inhibitor ibudilast (MN-166) has been marketed in Japan for over 25 years for
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Published 02 May 2017

Synthesis of ribavirin 2’-Me-C-nucleoside analogues

  • Fanny Cosson,
  • Aline Faroux,
  • Jean-Pierre Baltaze,
  • Jonathan Farjon,
  • Régis Guillot,
  • Jacques Uziel and
  • Nadège Lubin-Germain

Beilstein J. Org. Chem. 2017, 13, 755–761, doi:10.3762/bjoc.13.74

Graphical Abstract
  • carbon atom in the 2’-position are an indium-mediated alkynylation and a 1,3-dipolar cyclization. Keywords: alkynylation; antiviral; cancer; C-nucleosides; ribavirin; Introduction The triazole nucleoside ribavirin (RBV, Figure 1) is used for the treatment of a number of viral infections and may be
  • promising as an anticancer drug [1][2][3]. The antiviral activity of ribavirin is ascribed to a combination of different mechanisms [4]. Although RBV causes some side effects [5][6][7] essentially due to its accumulation in red blood cells, it is indispensable in the treatment against hepatitis C virus (HCV
  • if a bulkier ethyl group is used [16]. On the other hand, currently 2’-deoxy-2’-C-methyl-2’-C-fluoronucleosides are developed because a fluoro substituent in the 2’-position increases the antiviral activity and specificity due to a higher tolerance of viral polymerases with respect to incorporation
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Published 21 Apr 2017

Isoxazole derivatives as new nitric oxide elicitors in plants

  • Anca Oancea,
  • Emilian Georgescu,
  • Florentina Georgescu,
  • Alina Nicolescu,
  • Elena Iulia Oprita,
  • Catalina Tudora,
  • Lucian Vladulescu,
  • Marius-Constantin Vladulescu,
  • Florin Oancea and
  • Calin Deleanu

Beilstein J. Org. Chem. 2017, 13, 659–664, doi:10.3762/bjoc.13.65

Graphical Abstract
  • ; Introduction Isoxazoles are an interesting class of N-heterocyclic compounds intensely studied mainly due to their wide range of biological activity [1][2]. Isoxazole compounds show antiviral [3][4], antithrombotic [5][6][7][8][9], analgesic [9], COX-2 inhibitory [10][11], anti-inflamatory [9][11
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Published 06 Apr 2017

Synthesis of 1-indanones with a broad range of biological activity

  • Marika Turek,
  • Dorota Szczęsna,
  • Marek Koprowski and
  • Piotr Bałczewski

Beilstein J. Org. Chem. 2017, 13, 451–494, doi:10.3762/bjoc.13.48

Graphical Abstract
  • , have been performed. This review also covers the most important studies on the biological activity of 1-indanones and their derivatives which are potent antiviral, anti-inflammatory, analgesic, antimalarial, antibacterial and anticancer compounds. Moreover, they can be used in the treatment of
  • as antiviral and antibacterial agents [5] (I and II), anticancer drugs [6] (VI), pharmaceuticals used in the Alzheimer’s disease treatment [7] (III), cardiovascular drugs [7] (IV), insecticides, fungicides, herbicides [8] (V) and non-nucleoside, low molecular drugs for the hepatitis C treatment
  • allowed the synthesis of 60 in yields ranged from 31 to 56%. 1-Indanones exhibit a broad spectrum of biological activity including anti-inflammatory [41], analgesic [42], antimicrobial [43], antiviral [5], anticancer [44] and antimalarial [45] activity. A combination of two or more biologically active
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Published 09 Mar 2017

Revaluation of biomass-derived furfuryl alcohol derivatives for the synthesis of carbocyclic nucleoside phosphonate analogues

  • Bemba Sidi Mohamed,
  • Christian Périgaud and
  • Christophe Mathé

Beilstein J. Org. Chem. 2017, 13, 251–256, doi:10.3762/bjoc.13.28

Graphical Abstract
  • compounds were evaluated for their activity against a large number of viruses. However, none of them showed significant antiviral activity or cytotoxicity. Keywords: analogue; antiviral; carbocyclic; nucleoside; phosphonate; Introduction Biomass is a valuable resource in search of renewable organic carbon
  • some of the products have shown interesting antiviral activities. As part of our studies on carbocyclic nucleoside phosphonates [6] as potential anti-HIV agents [7][8], we envisioned to use bio-sourced racemic (+/−)-4-O-protected 2-cyclopentenone for the synthesis of hitherto unknown carbocyclic
  • nucleoside methylphosphonates (Figure 1) bearing purine bases (adenine and guanine) in order to evaluate their antiviral properties. Results and Discussion Synthesis of precursors (+/−)-5 and (+/−)-7 The synthesis began with the preparation of racemic 4-O-TBDMS-2-cyclopentenone (1) which was obtained in two
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Published 09 Feb 2017

Synthesis and evaluation of anti-oxidant and cytotoxic activities of novel 10-undecenoic acid methyl ester based lipoconjugates of phenolic acids

  • Naganna Narra,
  • Shiva Shanker Kaki,
  • Rachapudi Badari Narayana Prasad,
  • Sunil Misra,
  • Koude Dhevendar,
  • Venkateshwarlu Kontham and
  • Padmaja V. Korlipara

Beilstein J. Org. Chem. 2017, 13, 26–32, doi:10.3762/bjoc.13.4

Graphical Abstract
  • are a class of natural compounds which are found ubiquitously in the plant kingdom. They are reported to possess a wide range of biological properties like anti-oxidant, antimicrobial, anti-inflammatory, anticarcinogenic and antiviral activities [1]. The phenolic acids are also reported to show in
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Published 04 Jan 2017

Synthesis of acylhydrazino-peptomers, a new class of peptidomimetics, by consecutive Ugi and hydrazino-Ugi reactions

  • Angélica de Fátima S. Barreto,
  • Veronica Alves dos Santos and
  • Carlos Kleber Z. Andrade

Beilstein J. Org. Chem. 2016, 12, 2865–2872, doi:10.3762/bjoc.12.285

Graphical Abstract
  • compared to a natural peptide. Indeed, these compounds have shown to be a useful class of peptidomimetics with interesting biological activities [21][22][23], including antiviral [25][26] and cysteine protease inhibition [27][28][29][30]. Hydrazinopeptides [31][32][33][34][35][36] (peptide analogs in which
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Published 27 Dec 2016

Interactions between cyclodextrins and cellular components: Towards greener medical applications?

  • Loïc Leclercq

Beilstein J. Org. Chem. 2016, 12, 2644–2662, doi:10.3762/bjoc.12.261

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Published 07 Dec 2016

Enzymatic synthesis and phosphorolysis of 4(2)-thioxo- and 6(5)-azapyrimidine nucleosides by E. coli nucleoside phosphorylases

  • Vladimir A. Stepchenko,
  • Anatoly I. Miroshnikov,
  • Frank Seela and
  • Igor A. Mikhailopulo

Beilstein J. Org. Chem. 2016, 12, 2588–2601, doi:10.3762/bjoc.12.254

Graphical Abstract
  • antiviral activity in various experiments [15][16][17][18][19][20][21][22]. Regarding the chemical synthesis of this class of pyrimidine nucleosides various approaches were published (see, e.g., [8][9][10][11][14][15][16][23][24]; reviewed by Vorbrüggen and Ruh-Pohlenz [25]). On the contrary, only few
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Published 01 Dec 2016
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