Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

• Allison S. Limpert,
• Margrith E. Mattmann and
• Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

• characterized in ALS, including, but not limited to glutamate toxicity, protein misfolding and aggregation, endoplasmic reticulum (ER) stress, loss of trophic factors, oxidative stress, inflammation, disrupted protein trafficking, and mitochondrial dysfunction [5]. Therapeutic development has been based around

• with GSK-3 inhibitors reduced markers of inflammation in the spinal cord [63], suggesting a reduction in glial reactivity. Reduction in oxidative stress and inflammation Another hallmark of ALS is chronic neuronal exposure to oxidative stress and inflammation and thus several treatment strategies are

• , oxidative stress, inflammation, and mitochondrial dysfunction. Although some cases of ALS can be attributed to known gene mutations, the cause of ALS remains largely undefined. Therefore, current treatment strategies for ALS involve the targeting of specific cellular dysfunctions. As mutations in the SOD1

End-labeled amino terminated monotelechelic glycopolymers generated by ROMP and Cu(I)-catalyzed azide–alkyne cycloaddition

• Ronald Okoth and
• Amit Basu

Beilstein J. Org. Chem. 2013, 9, 608–612, doi:10.3762/bjoc.9.66

• cyclooctenes have been used to examine the role of glycans in such processes such as neurite outgrowth [4], bacterial motility [5], and inflammation [6]. ROMP polymers with pendant reactive functional groups, such as N-hydroxysuccinimide (NHS) or nitrophenyl esters, are useful materials since the pendant

Towards a biocompatible artificial lung: Covalent functionalization of poly(4-methylpent-1-ene) (TPX) with cRGD pentapeptide

• Lena Möller,
• Christian Hess,
• Jiří Paleček,
• Yi Su,
• Axel Haverich,
• Andreas Kirschning and
• Gerald Dräger

Beilstein J. Org. Chem. 2013, 9, 270–277, doi:10.3762/bjoc.9.33

• treatment is conducted when patients respond inadequately to medical therapy. However, invasive mechanical ventilation can damage the lungs physically by overpressurizing lung tissue or due to inflammation. This may lead to exacerbation of lung dysfunction or even to multiple-organ failure [2][3]. The

Cyclodextrin-based nanosponges as drug carriers

• Francesco Trotta,
• Marco Zanetti and
• Roberta Cavalli

Beilstein J. Org. Chem. 2012, 8, 2091–2099, doi:10.3762/bjoc.8.235

• and prolonged ASA release from pyromellitic cross-linked β-cyclodextrin nanosponges over a long period, i.e., 24 hours. In carrageenan-induced rat paw edema, administration of ASA as a nanosponge formulation administered by oral gavage reduced inflammation significantly (P < 0.01 and P < 0.05

Enantioselective total synthesis of (R)-(−)-complanine

• Krystal A. D. Kamanos and
• Jonathan M. Withey

Beilstein J. Org. Chem. 2012, 8, 1695–1699, doi:10.3762/bjoc.8.192

• complanata, and known to be a causative agent in inflammation. An organocatalytic, asymmetric oxyamination of a homoconjugated all-Z-dienal intermediate provides versatile and efficient access to the natural product. Keywords: complanine; enantioselective synthesis; marine fireworm; nitrosoaldol

• ; organocatalysis; Introduction The marine fireworm Eurythoe complanata resides in the shallow water and sands of temperate and sub-tropical regions. Its small setae cause skin inflammation upon contact, the causative agent having been identified as complanine. This novel amphipathic substance was first isolated

• from Eurythoe complanata in 2008, by Nakamura and Uemura [1]. Complanine induces inflammation by activating PKC (protein kinase C) in the presence of Ca2+ and TPA (12-O-tetradecanoylphorbol 13-acetate). PKC plays an important role in inflammation, namely through control of signal transduction cascades

Automated synthesis of sialylated oligosaccharides

• Davide Esposito,
• Mattan Hurevich,
• Bastien Castagner,
• Cheng-Chung Wang and
• Peter H. Seeberger

Beilstein J. Org. Chem. 2012, 8, 1601–1609, doi:10.3762/bjoc.8.183

• been implicated in inflammation and cancer metastasis [26], and was chosen as a model glycan for the construction of branched compounds. Glucosamine building block 23, containing C3-levulinoyl (Lev) and C4-Fmoc protecting groups [27], was first reacted with the linker. The glycosylation was followed by

High-affinity multivalent wheat germ agglutinin ligands by one-pot click reaction

• Henning S. G. Beckmann,
• Heiko M. Möller and
• Valentin Wittmann

Beilstein J. Org. Chem. 2012, 8, 819–826, doi:10.3762/bjoc.8.91

• ; cluster effect; lectins; multivalency; Introduction The recognition of carbohydrate structures by carbohydrate binding proteins (lectins) plays a fundamental role in numerous intra- and intercellular events during development, inflammation, immune response, cancer metastasis, and pathogen–host

Synthetic glycopeptides and glycoproteins with applications in biological research

• Ulrika Westerlind

Beilstein J. Org. Chem. 2012, 8, 804–818, doi:10.3762/bjoc.8.90

• cell-surface binding events, such as cell growth and differentiation, cell proliferation, cell adhesion, binding of pathogens, fertilization and immune responses [1][2]. Furthermore, glycans assist in intracellular protein folding and transport. Pathogenic processes, such as chronic inflammation, viral

• distance (Figure 2) [140][141][142]. In another study, a combinatorial library of fucosyl-peptide dendrimers was synthesized and screened for binding to the fucose-specific lectin (LecB) from Pseudomonas aeruginosa, a pathogen causing severe infections in patients leading to chronic inflammation in the

Triterpenoid saponins from the roots of Acanthophyllum gypsophiloides Regel

• Elena A. Khatuntseva,
• Vladimir M. Men’shov,
• Alexander S. Shashkov,
• Yury E. Tsvetkov,
• Rodion N. Stepanenko,
• Raymonda Ya. Vlasenko,
• Elvira E. Shults,
• Genrikh A. Tolstikov,
• Tatjana G. Tolstikova,
• Dimitri S. Baev,
• Vasiliy A. Kaledin,
• Nelli A. Popova,
• Valeriy P. Nikolin,
• Pavel P. Laktionov,
• Anna V. Cherepanova,
• Tatiana V. Kulakovskaya,
• Ekaterina V. Kulakovskaya and
• Nikolay E. Nifantiev

Beilstein J. Org. Chem. 2012, 8, 763–775, doi:10.3762/bjoc.8.87

• nature of compounds 1 and 2, the presence of glucuronic acid at C-3 of the aglycone, and the absence of a lipid moiety. Histamine-induced acute inflammation in the paws of the mice was used as a classical model of edema formation for the study of the anti-inflammatory activity of saponins. Two methods of

• saponins are not able to induce an innate immune response in endothelium. Thus we can conclude that compounds 1 and 2 are not prone to cause inflammation of the vessel endothelium. To estimate the adjuvant properties of compounds 1 and 2 a series of test immunizations was carried out by using the synthetic

• inflammation in the vessel endothelium. Meanwhile, compounds 1 and 2 exhibited prominent immune-stimulating properties and can be considered as a prospective adjuvant in combination with KLH-based neoglycoconjugates. The antifungal activity of saponins 1 and 2 was also examined on four yeast species

2-Allylphenyl glycosides as complementary building blocks for oligosaccharide and glycoconjugate synthesis

• Hemali D. Premathilake and
• Alexei V. Demchenko

Beilstein J. Org. Chem. 2012, 8, 597–605, doi:10.3762/bjoc.8.66

• in recent years, we have already learned that carbohydrates are involved in a broad range of vital biological processes (e.g., fertilization, anti-inflammation, immunoresponse, joint lubrication, antigenic determination) [1]. Carbohydrates are also involved in many harmful processes (e.g., bacterial

Manganese dioxide mediated one-pot synthesis of methyl 9H-pyrido[3,4-b]indole-1-carboxylate: Concise synthesis of alangiobussinine

• Jessica Baiget,
• Sabin Llona-Minguez,
• Stuart Lang,
• Simon P. MacKay,
• Colin J. Suckling and
• Oliver B. Sutcliffe

Beilstein J. Org. Chem. 2011, 7, 1407–1411, doi:10.3762/bjoc.7.164

• important class of naturally occurring compounds containing the β-carboline motif found in a number of biologically active molecules, and which have recently been shown to be active against Alzheimer’s disease [1][2], bacterial infection [3], inflammation [4][5], HIV and AIDS [6] and various forms of

Novel synthesis of pseudopeptides bearing a difluoromethyl group by Ugi reaction and desulfanylation

• Jingjing Wu,
• Hui Li and
• Song Cao

Beilstein J. Org. Chem. 2011, 7, 1070–1074, doi:10.3762/bjoc.7.123

• reported of the preparation and bioassay of pseudopeptides and peptidomimetics bearing difluoromethyl groups. For example, compound I can act as bradykinin B1 antagonist or inverse agonist and can be used in the prevention of inflammation and pain [19]. Compound II is an inhibitor of microsomal

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

• have also been reported, however, these usually rely on longer reaction sequences and require more expensive starting materials (Scheme 30) [42][43]. Etodolac (153, Lodine) is a racemic non-steroidal anti-inflammatory tetrahydrocarbazole derivative used to treat inflammation and prescribed for general

Bioorthogonal metabolic glycoengineering of human larynx carcinoma (HEp-2) cells targeting sialic acid

• Arne Homann,
• Riaz-ul Qamar,
• Sevnur Serim,
• Petra Dersch and
• Jürgen Seibel

Beilstein J. Org. Chem. 2010, 6, No. 24, doi:10.3762/bjoc.6.24

• processes involved in infection, inflammation or tumor formation [1]. Recent studies have shown that the surface of a T-cell line (Jurkat), Chinese hamster ovary (CHO) cells, cervical adenocarcinoma (HeLa) cells as well as many other cell types can be labelled with bioorthogonal, that is metabolically inert

(−)-Complanine, an inflammatory substance of marine fireworm: a synthetic study

• Kazuhiko Nakamura,
• Yu Tachikawa and
• Daisuke Uemura

Beilstein J. Org. Chem. 2009, 5, No. 12, doi:10.3762/bjoc.5.12

• substance is thought to be used as part of the animal’s defense system. In a previous study the molecular mechanism of inflammation by the action of complanine was examined, and its activation of protein kinase C (PKC) in the presence of Ca2+ and 12-O-tetradecanoylphorbol 13-acetate (TPA) has been proved

• . These results suggest that complanine can bind PKC at the same site as phosphatidylserine, a co-activation factor with Ca2+ and TPA. It is known that signal transduction leads to an inflammation mediator TNF-α and its downstream signal molecules, which occurs by phosphorylation through the action of PKC

ADDP and PS-PPh₃: an efficient Mitsunobu protocol for the preparation of pyridine ether PPAR agonists

• Paul S. Humphries,
• Quyen-Quyen T. Do and
• David M. Wilhite

Beilstein J. Org. Chem. 2006, 2, No. 21, doi:10.1186/1860-5397-2-21

• pathways for lipid handling, insulin sensitivity, inflammation and other functions have led to marketed drugs and vast clinical and preclinical research efforts.[1][2][3][4][5][6][7][8][9][10][11] In 1991, a series of PPAR analogues were disclosed, which for the first time did not contain a thiazolidine