Structure/affinity studies in the bicyclo-DNA series: Synthesis and properties of oligonucleotides containing bc^en-T and iso-tricyclo-T nucleosides

• Branislav Dugovic,
• Michael Wagner and
• Christian J. Leumann

Beilstein J. Org. Chem. 2014, 10, 1840–1847, doi:10.3762/bjoc.10.194

• ]. Duplexes with RNA as complement are also destabilized albeit to a lesser extent (ΔTm/mod −0.8 to −2.2 °C). The same sequence dependence as for DNA as complement appears and again, two consecutive modifications are associated with the least depression in Tm/modification. Thus, it turns out that bcen-DNA

Stereocontrolled synthesis of 5-azaspiro[2.3]hexane derivatives as conformationally “frozen” analogues of L-glutamic acid

• Beatrice Bechi,
• David Amantini,
• Cristina Tintori,
• Maurizio Botta and
• Romano di Fabio

Beilstein J. Org. Chem. 2014, 10, 1114–1120, doi:10.3762/bjoc.10.110

• -glutamic acid (L-Glu, 1) is of particular importance since it is the primary excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a critical role in a wide range of disorders like schizophrenia, depression, neurodegenerative diseases such as Parkinson’s and Alzheimer’s and in

• coupled or metabotropic glutamate receptors (mGluRs) [6][7]. To date, eight different metabotropic receptor subtypes (mGluR1–8) have been identified. Compounds that modulate the function of the mGluRs might be useful for treating a wide range of CNS disorders including schizophrenia, depression, anxiety

End-group-functionalized poly(N,N-diethylacrylamide) via free-radical chain transfer polymerization: Influence of sulfur oxidation and cyclodextrin on self-organization and cloud points in water

• Sebastian Reinelt,
• Daniel Steinke and
• Helmut Ritter

Beilstein J. Org. Chem. 2014, 10, 680–691, doi:10.3762/bjoc.10.61

• regarding the cloud point depression of thermoresponsive polymers containing hydrophobic end-groups with decreasing molecular weight [20][24][30][44] or the effect of an increasing hydrophobic environment in amphiphilic conetworks [45] are in accordance with previous studies. Theoretically a stronger

Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics

• Gijs Koopmanschap,
• Eelco Ruijter and
• Romano V.A. Orru

Beilstein J. Org. Chem. 2014, 10, 544–598, doi:10.3762/bjoc.10.50

• numerous pharmaceutical and biological active compounds. For example, they are found in compounds used for the treatment of epilepsy [65][66], HIV [67][68], and depression [69]. Multicomponent reactions towards γ-lactam peptidomimetics were earlier described by Ugi [70], Mjalli [71] and Harriman [72

Automated three-component synthesis of a library of γ-lactams

• Erik Fenster,
• David Hill,
• Oliver Reiser and
• Jeffrey Aubé

Beilstein J. Org. Chem. 2012, 8, 1804–1813, doi:10.3762/bjoc.8.206

• been significant in the treatment of epilepsy [6][7], HIV [8][9], neurodegenerative disease and depression [10][11]. Having identified the lactam ring as a target of opportunity in chemical-screening efforts, we previously reported a method to prepare γ-lactams from readily available maleimides

Antifreeze glycopeptide diastereomers

• Lilly Nagel,
• Carsten Budke,
• Axel Dreyer,
• Thomas Koop and
• Norbert Sewald

Beilstein J. Org. Chem. 2012, 8, 1657–1667, doi:10.3762/bjoc.8.190

• ; ice recrystallization; microwave chemistry; Introduction Several fish species living in polar and subpolar oceans have developed a strategy to survive in water at an average temperature of −1.8 °C. This non-colligative freezing-point depression is based on the prevention of ice growth in

Palladium- and copper-mediated N-aryl bond formation reactions for the synthesis of biological active compounds

• Carolin Fischer and
• Burkhard Koenig

Beilstein J. Org. Chem. 2011, 7, 59–74, doi:10.3762/bjoc.7.10

• synthesis of an atropisomeric N-(2-tert-butylphenyl)lactam as an intermediate for norepinephrine transporter (NET) inhibitor 16. NET inhibitors were developed to treat a variety of mental disorders such as depression and attention deficit hyperactivity disorder (ADHD). Screening different ligands, SERGPHOS

8-epi-Salvinorin B: crystal structure and affinity at the κ opioid receptor

• Thomas A. Munro,
• Katharine K. Duncan,
• Richard J. Staples,
• Wei Xu,
• Lee-Yuan Liu-Chen,
• Cécile Béguin,
• William A. Carlezon Jr. and
• Bruce M. Cohen

Beilstein J. Org. Chem. 2007, 3, No. 1, doi:10.1186/1860-5397-3-1

• stability or solubility.[7] Others have increased affinity and potency, [8] or altered subtype selectivity.[9] As yet, however, no derivatives of 1a appear to be KOR partial agonists or antagonists, classes of agents that may have utility in the treatment of psychiatric conditions such as depression or