Diversity-Oriented Synthesis of Natural-Product-like Libraries Containing a 3-Methylbenzofuran Moiety for the Discovery of New Chemical Elicitors.

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.

A pH-responsive fluorescent [5]pseudorotaxane formed by self-assembly of cationic water-soluble pillar[5]arenes and a tetraphenylethene derivative.

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.

Tubular Structures Self-Assembled from a Bola-Amphiphilic Pillar[5]arene in Water and Applied as a Microreactor.

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.

P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.

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.