- CLICKable azide-functionalized phosphonates for the surface-modification of molecular and solid-state metal oxides
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The covalent functionalization of metal oxide surfaces with organic ligands gives unique organic-inorganic hybrids. Here we report a bifunctional organic tether combining a phosphonate for metal oxide anchoring with an organic azide for attachment of organic groups. Stable binding of the tether to molecular and solid-state metal oxides is demonstrated and the subsequent CLICKability of the TiO2-anchored tether is shown. The phosphonate-azide reported could in future allow the general linkage of functional organic groups to metal oxides.
- Sch?nweiz,Knoll,Anjass,Braumüller,Rau,Streb
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- Designing anti-inflammatory drugs from parasitic worms: A synthetic small molecule analogue of the acanthocheilonema viteae product ES-62 prevents development of collagen-induced arthritis
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In spite of increasing evidence that parasitic worms may protect humans from developing allergic and autoimmune diseases and the continuing identification of defined helminth-derived immunomodulatory molecules, to date no new anti-inflammatory drugs have been developed from these organisms. We have approached this matter in a novel manner by synthesizing a library of drug-like small molecules based upon phosphorylcholine, the active moiety of the anti-inflammatory Acanthocheilonema viteae product, ES-62, which as an immunogenic protein is unsuitable for use as a drug. Following preliminary in vitro screening for inhibitory effects on relevant macrophage cytokine responses, a sulfone-containing phosphorylcholine analogue (11a) was selected for testing in an in vivo model of inflammation, collagen-induced arthritis (CIA). Testing revealed that 11a was as effective as ES-62 in protecting DBA/1 mice from developing CIA and mirrored its mechanism of action in downregulating the TLR/IL-1R transducer, MyD88. 11a is thus a novel prototype for anti-inflammatory drug development.
- Al-Riyami, Lamyaa,Pineda, Miguel A.,Rzepecka, Justyna,Huggan, Judith K.,Khalaf, Abedawn I.,Suckling, Colin J.,Scott, Fraser J.,Rodgers, David T.,Harnett, Margaret M.,Harnett, William
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p. 9982 - 10002
(2014/01/17)
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