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

• because of their potential as drug candidates for the treatment of Alzheimer’s disease [14][15][16][17]. To effectively generate muscarine analogues from AnGal, an adequate strategy for the placement of an exocyclic amino group attached to the C-threofuranose ring is required. Because of the presence of

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

• 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

• -indanone derivatives 66 were obtained in 13–86% yields (Scheme 22). This method was further applied to the synthesis of biologically active compounds, such as 1-tetralones, 1-benzosuberones and donepezil (a potent acetylcholinesterase inhibitor used in the treatment of Alzheimer’s disease). Halo-1

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

• topics including cholesterol manipulation, treatment of Alzheimer’s disease, control of pathogens, etc. In addition, the use of natural CDs offers the great advantage of avoiding or reducing the use of common petroleum-sourced drugs. In this paper, the general features and applications of CDs have been

Inhibition of peptide aggregation by means of enzymatic phosphorylation

• Kristin Folmert,
• Malgorzata Broncel,
• Hans v. Berlepsch,
• Christopher H. Ullrich,
• Mary-Ann Siegert and
• Beate Koksch

Beilstein J. Org. Chem. 2016, 12, 2462–2470, doi:10.3762/bjoc.12.240

• ][29]. Phosphorylation caused by abnormal activities of phosphatases and/or kinases is associated with known diseases such as cancer [30], multiple sclerosis [31], diabetes [32] and Alzheimer’s disease [33]. The accumulation of hyperphosphorylated tau protein as trigger for several dementias was

Unconventional application of the Mitsunobu reaction: Selective flavonolignan dehydration yielding hydnocarpins

• Guozheng Huang,
• Simon Schramm,
• Jörg Heilmann,
• David Biedermann,
• Vladimír Křen and
• Michael Decker

Beilstein J. Org. Chem. 2016, 12, 662–669, doi:10.3762/bjoc.12.66

• , our group has developed a hybrid drug combining silibinin with tacrine (a potent acetylcholinesterase inhibitor for treatment of Alzheimer’s disease), which shows neuro- and hepatoprotective effects exceeding the cytoprotective effects of silibinin and effectively counteracts tacrine’s dose-dependent

Biosynthesis of α-pyrones

• Till F. Schäberle

Beilstein J. Org. Chem. 2016, 12, 571–588, doi:10.3762/bjoc.12.56

• interesting target of research, due to the fact that the progression of Alzheimer’s disease was slowed down by using anti-inflammatory drugs. Thus, selective COX-2 inhibitors, anti-inflammatory compounds themselves, might have beneficial effects in vivo. Several derivatives of 6-alkyl (alkoxy or alkylthio)-4

Self and directed assembly: people and molecules

• Tony D. James

Beilstein J. Org. Chem. 2016, 12, 391–405, doi:10.3762/bjoc.12.42

• receptors that is currently emerging is in the measurement of protein glycation. Glycated proteins are potentially important biomarkers for sugar-related non-communicable disease states, such as atherosclerosis, autoimmune diseases, cancer, and Alzheimer’s disease (AD). Some researchers have even coined the

• improve in the efficiency of treatment strategies. The two examples given above, one for the home and closed loop treatment of diabetes and the other for a simple diagnostic test for Alzheimer’s disease (AD), clearly demonstrate that the near future of boronic acid based receptor research is assured. What

Assembly of synthetic Aβ miniamyloids on polyol templates

• Sebastian Nils Fischer and
• Armin Geyer

Beilstein J. Org. Chem. 2015, 11, 2646–2653, doi:10.3762/bjoc.11.284

• formation [2]. Alternatively, it is started by seeding with amyloid fragments whose large surface-to-core ratio greatly accelerates the fibril formation. Although amyloid structures are well studied in vitro, their in vivo relevance at the onset of Alzheimer’s disease remains under debate [3]. Aβ peptides

Synthesis, antimicrobial and cytotoxicity evaluation of new cholesterol congeners

• Mohamed Ramadan El Sayed Aly,
• Hosam Ali Saad and
• Shams Hashim Abdel-Hafez

Beilstein J. Org. Chem. 2015, 11, 1922–1932, doi:10.3762/bjoc.11.208

• (V), were used to prepare nontoxic unilamellar vesicles as nanocarriers for gene delivery into Neuro2A cells, which are involved in neurodegenerative diseases [19]. Also, the involvement of cholesterol metal ion complexes in Alzheimer’s disease was reviewed [20]. Cholesterol glycosides are known for

4-Hydroxy-6-alkyl-2-pyrones as nucleophilic coupling partners in Mitsunobu reactions and oxa-Michael additions

• Michael J. Burns,
• Thomas O. Ronson,
• Richard J. K. Taylor and
• Ian J. S. Fairlamb

Beilstein J. Org. Chem. 2014, 10, 1159–1165, doi:10.3762/bjoc.10.116

• functionalised 2-pyrones have been identified as promising candidates for the treatment of illnesses ranging from Alzheimer’s disease [3] to cancer [4]. An important sub-class of pyrones are the 4-hydroxy-2-pyrones, which are sometimes found embedded into larger natural products as pyronyl ethers, such as in the

Synthesis of the tetracyclic core of Illicium sesquiterpenes using an organocatalyzed asymmetric Robinson annulation

• Lynnie Trzoss,
• Jing Xu,
• Michelle H. Lacoske and
• Emmanuel A. Theodorakis

Beilstein J. Org. Chem. 2013, 9, 1135–1140, doi:10.3762/bjoc.9.126

• the treatment of various neurodegenerative diseases including Alzheimer’s disease [4] and Parkinson’s disease [5]. Despite their unambiguous importance, approaches to neurotrophin-based drug development have encountered problems associated with their limited oral availability, insufficient delivery to

Amyloid-β probes: Review of structure–activity and brain-kinetics relationships

• Todd J. Eckroat,
• Abdelrahman S. Mayhoub and
• Sylvie Garneau-Tsodikova

Beilstein J. Org. Chem. 2013, 9, 1012–1044, doi:10.3762/bjoc.9.116

• Ave, Ann Arbor, MI, 48109-2216, United States 10.3762/bjoc.9.116 Abstract The number of people suffering from Alzheimer’s disease (AD) is expected to increase dramatically in the coming years, placing a huge burden on society. Current treatments for AD leave much to be desired, and numerous research

• relationships with regards to affinity for target and brain kinetics. Several probes discussed herein show particularly promising results and will be of immense value moving forward in the fight against AD. Keywords: Alzheimer’s disease; in vivo detection; near-infrared fluorescence probes; PET/SPECT imaging

• ; radioactive probes; Introduction Alzheimer’s disease (AD) is a progressive neurodegenerative disorder of the central nervous system currently affecting ~5.4 million Americans, a number that could increase to 11–16 million by the year 2050. In the United States, AD represents the 6th leading cause of death

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

• ], Charcot Marie Tooth disease [80], Alzheimer’s disease [81], and Huntington’s disease [82]. The discovery of small molecules that prevent or clear protein aggregates may prove to be valuable for the treatment of multiple disorders. Another common strategy for the treatment of ALS is the use of compounds

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

Continuous flow photolysis of aryl azides: Preparation of 3H-azepinones

• Farhan R. Bou-Hamdan,
• François Lévesque,
• Alexander G. O'Brien and
• Peter H. Seeberger

Beilstein J. Org. Chem. 2011, 7, 1124–1129, doi:10.3762/bjoc.7.129

• -azidoterephthalate (8d) each reacted favorably compared to the model substrate 8a. We were particularly interested in the preparation of 5-aryl-3H-azepinones 9e–g, examples of which have seen recent interest as γ-secretase inhibitors for the treatment of Alzheimer’s disease [37]. Photolysis of methyl 2-azido-5

Synthesis and enzymatic evaluation of 2- and 4-aminothiazole- based inhibitors of neuronal nitric oxide synthase

• Graham R. Lawton,
• Haitao Ji,
• Pavel Martásek,
• Linda J. Roman and
• Richard B. Silverman

Beilstein J. Org. Chem. 2009, 5, No. 28, doi:10.3762/bjoc.5.28

• constitutive isoform of nitric oxide synthase (NOS) found in the CNS. It is believed to play a role in many neurological diseases, including Parkinson’s disease [1], Alzheimer’s disease [2], damage due to stroke [3], and cerebral palsy caused by pre-natal hypoxia [4]. To fully explore the role nNOS plays in