Archive for August, 2009

Graphical contents list

Publication year: 2009
Source: Bioorganic & Medicinal Chemistry, Volume 17, Issue 18, 15 September 2009, Pages 6481-6490
[No author name available]

Editorial board

Publication year: 2009
Source: Bioorganic & Medicinal Chemistry, Volume 17, Issue 18, 15 September 2009, Page IFC
[No author name available]

Design, synthesis and evaluation of monovalent ligands for the asialoglycoprotein receptor (ASGP-R)

Publication year: 2009
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 29 August 2009
Daniela, Stokmaier , Oleg, Khorev , Brian, Cutting , Rita, Born , Daniel, Ricklin , …

A series of novel aryl-substituted triazolyl D-galactosamine derivatives was synthesized as ligands for the carbohydrate recognition domain of the major subunit H1 (H1-CRD) of the human asialoglycoprotein receptor (ASGP-R). The compounds were biologically evaluated with a newly developed competitive binding assay, surface plasmon resonance and by a competitive NMR binding experiment. With compound 1b, a new ligand with a two-fold improved affinity to the best so far known D-GalNAc was identified. This small, drug-like ligand can be used as targeting device for drug delivery to hepatocytes.

Hepatoprotective amide constituents from the fruit of Piper chaba: structural requirements, mode of action, and new amides

Publication year: 2009
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 29 August 2009
Hisashi, Matsuda , Kiyofumi, Ninomiya , Toshio, Morikawa , Daisuke, Yasuda , Itadaki, Yamaguchi , …

The 80% aqueous acetone extract from the fruit of Piper chaba (Piperaceae) was found to have hepatoprotective effects on D-galactosamine (D-GalN)/lipopolysaccharide-induced liver injury in mice. From the ethyl acetate-soluble fraction, three new amides, piperchabamides E, G, and H, 33 amides, and four aromatic constituents were isolated. Among the isolates, several amide constituents inhibited D-GalN/tumor necrosis factor-a (TNF-a)-induced death of hepatocytes, and the following structural requirements were suggested: i) the amide moiety is essential for potent activity; and ii) the 1,9-decadiene structure between the benzene ring and the amide moiety tended to enhance the activity. Moreover, a principal constituent, piperine, exhibited…

Efficient and Diverse Synthesis of Indole Derivatives

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6895-6898, September 4, 2009.

Chiral Bro̷nsted Acid-Catalyzed Asymmetric Friedel−Crafts Alkylation of Pyrroles with Nitroolefins

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6899-6901, September 4, 2009.

Efficient Total Synthesis of (−)-cis-Clavicipitic Acid

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6859-6862, September 4, 2009.

The Base-Catalyzed Keto−Enol Interconversion of 2-Nitrocyclohexanone in Ionic Liquids

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6572-6576, September 4, 2009.

A Chemistry Cascade: From Physical Organic Studies of Alkoxy Radicals to Alkaloid Synthesis†

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6421-6441, September 4, 2009.

Efficient Regioselective Synthesis of Indole N-Carboximidamides and N-Carboximidoates by a Sequential Aza-Wittig/Ag(I)-Catalyzed Cyclization

The Journal of Organic Chemistry, Volume 74, Issue 17, Page 6874-6877, September 4, 2009.