953044-12-7Relevant academic research and scientific papers
Dehydrative cyclization catalyzed by the combination of molybdenum(VI) oxides and benzoic acids: First synthesis of the antitumour substance BE-70016
Sakakura, Akira,Umemura, Shuhei,Kondo, Rei,Ishihara, Kazuaki
, p. 551 - 555 (2007)
The dehydrative cyclization of N-(o-hydroxybenzoyl)threonine derivative la is efficiently promoted by the combined use of molybdenum(VI) oxides and benzoic acids bearing electron-with-drawing substituents. In the presence of ammonium molybdate [(NH4
Total Synthesis of the Proposed Structure of Mycobactin J
Ghosh, Chiranjit,Pal, Sujit,Patel, Akanksha,Kapur, Manmohan
supporting information, p. 6511 - 6515 (2018/10/20)
The total synthesis of the proposed structure of mycobactin J (MJ), a metabolite of Mycobacterium tuberculosis, is presented. The highlights of the synthesis include a careful control of the Z-stereochemistry of the unsaturated long chain fatty acid, a biomimetic construction of the oxazoline building block and the carriage of an unprotected phenol throughout the synthesis.
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products
Lin, Zhenjian,Smith, Misty D.,Concepcion, Gisela P.,Haygood, Margo G.,Olivera, Baldomero M.,Light, Alan,Schmidt, Eric W.
, p. 2360 - 2370 (2017/09/01)
Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure-activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore. Tests in mice show potential antiseizure and antinociceptive activities at high doses without motor impairment.
