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1.
ChemistryOpen ; 6(1): 102-111, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28168155

RESUMO

Natural products are a major source of biological molecules. The 3-methylfuran scaffold is found in a variety of plant secondary metabolite chemical elicitors that confer host-plant resistance against insect pests. Herein, the diversity-oriented synthesis of a natural-product-like library is reported, in which the 3-methylfuran core is fused in an angular attachment to six common natural product scaffolds-coumarin, chalcone, flavone, flavonol, isoflavone and isoquinolinone. The structural diversity of this library is assessed computationally using cheminformatic analysis. Phenotypic high-throughput screening of ß-glucuronidase activity uncovers several hits. Further in vivo screening confirms that these hits can induce resistance in rice to nymphs of the brown planthopper Nilaparvata lugens. This work validates the combination of diversity-oriented synthesis and high-throughput screening of ß-glucuronidase activity as a strategy for discovering new chemical elicitors.

2.
Org Lett ; 17(17): 4160-3, 2015 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-26275020

RESUMO

Various nanomorphologies were obtained by simply changing the fabrication conditions, such as the pH of the system, different solvent, or different concentration, of bola-amphiphilic pillar[5]arene Bola-AP5. Importantly, hybrid microtubules as a microreactor were successfully prepared by directly reducing AuCl4(-) on the surface of Bola-AP5-based tubular structures in water.

3.
Chem Commun (Camb) ; 51(61): 12220-3, 2015 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-26134923

RESUMO

The formation of a pH-responsive fluorescent [5]pseudorotaxane by self-assembly of cationic water-soluble pillar[5]arenes and a tetraphenylethene derivative was reported.

4.
Bioorg Med Chem Lett ; 16(15): 3960-5, 2006 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-16730985

RESUMO

Synthesis and HCV NS3 serine protease inhibitory activity of 4-hydroxyproline derived macrocyclic inhibitors and SAR around this macrocyclic core is described in this communication. X-ray structure of inhibitor 38 bound to the protease is discussed.


Assuntos
Hepatite C/enzimologia , Compostos Macrocíclicos/farmacologia , Inibidores de Serina Proteinase/farmacologia , Proteínas não Estruturais Virais/antagonistas & inibidores , Difração de Raios X
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