• Title/Summary/Keyword: Bis-${\gamma}$-butyrolactone

Search Result 2, Processing Time 0.014 seconds

Conformationally Constrained Analogues of Diacylglycerol Having a Perhydrofuro[3,4-c]furan-1,4-dione Bis-${\gamma}$-butyrolactone Skeleton

  • Lee, Jee-Woo;Nancy-E. Lewin;Peter-M. Blumberg;Victor-E. Marquez
    • Archives of Pharmacal Research
    • /
    • v.21 no.2
    • /
    • pp.164-167
    • /
    • 1998
  • Bis-${\gamma}$-lactones (1,2) having a perhydrofuro[3,4-c]furan-1,4-dione skeleton were designed as conformationally constrained diacylglycerol analogues. They were synthesized from D-apiose in 11 steps, and evaluated as $PKC-{\alpha}$ ligands by measuring their ability to displace bound $^3H$]PDBU from the enzyme. The compounds showed moderate binding affinities with $K_i$ values of 13.89 (${\pm}5.67$) ${\mu}M$ and 11.47 (${\pm}0.89$) ${\mu}M$, respectively. Their similar binding affinities indicate that these two bicyclic compounds were not effectively discriminated by $PKC-{\alpha}$ in terms of the direction of the side chain as other ligands built on similar bis-${\gamma}$-lactones.

  • PDF

Synthesis of Rosinimide Modified with Polyphenylpyridinylsiloxane and Its Characteristics

  • Kang, Doo-Whan;Kim, Young-Min
    • Fibers and Polymers
    • /
    • v.1 no.2
    • /
    • pp.67-70
    • /
    • 2000
  • Rosin maleic anhydride adduct (RMA)-bisester was prepared by the esterification of chlorinated RMA with hydroquinone. Phenylpyridinylcyclot.isiloxane ($D_3^{Ph,Py}$) was synthesized from phenylpyridinyldichlorosilane in the presence of zinc oxide catalyst, and amino group terminated polyphenylpyridinylsiloxane prepolymer was prepared by equilibrium polymerization of $D_3^{Ph,Py}$ with 1,3-bis(3-aminopropyl)-1,1,3,3-tetramethyldisiloxane. Rosinimide (PSMR) was prepared from the imidization of RMA-bisester with polyphenylpyridinylsiloxane prepolymer at 12$0^{\circ}C$ for 7 h using ${\gamma}$-butyrolactone/pyridine. It showed that PSMR had better thermal stalbility than rosinimide modified with polydimethylsiloxane.

  • PDF