The catalytic efficiency in organic synthesis of the aqueous extract of the pericarp of Sapindus trifoliatus fruits was evaluated. The synthesis of a series of aldimines from aromatic aldehydes and amines was successfully catalyzed by the extract, whereas aromatic ketones and amines did not yield ketimines under comparable reaction conditions, indicating the chemoselective catalysis of the extract
Triazolines. 14. 1,2,3-Triazolines and triazoles. A new class of anticonvulsants. Drug design and structure-activity relationships
作者:Pankaja K. Kadaba
DOI:10.1021/jm00396a032
日期:1988.1
could be linked to their chemistry or structural conformation. The triazolines and triazoles evince anticonvulsant activity as a class and compare very well with the prototype antiepileptic drugs--ethosuximide, phenytoin, phenobarbital, valproate--in their anticonvulsant potency and minimal neurotoxicity. They have emerged as a new generation of anticonvulsant agents that show great promise as potentially
demonstrated, and this tunable fluorescence was further used to study the re‐composition of a solid film. Moreover, the dynamic covalent films also exhibited responsiveness to competing amines and acid/base conditions, both in solutions and solid film–solution interface. This work can provide more insights into interface dynamicchemistry and holds great potential for further applications in optical and biomedical
Development of Novel Vitamin D Receptor–Coactivator Inhibitors
作者:Preetpal S. Sidhu、Nicholas Nassif、Megan M. McCallum、Kelly Teske、Belaynesh Feleke、Nina Y. Yuan、Premchendar Nandhikonda、James M. Cook、Rakesh K. Singh、Daniel D. Bikle、Leggy A. Arnold
DOI:10.1021/ml400462j
日期:2014.2.13
Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation, and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves. like a VDR antagonist by repressing 1,25-(OH)(2)D-3 activated gene transcription. In addition, PS121912 induced apoptosis in HL-60.