Combinatorial Discovery of Fluorescent Pharmacophores by Multicomponent Reactions in Droplet Arrays
作者:Olga N. Burchak、Laurent Mugherli、Mariano Ostuni、Jean Jacques Lacapère、Maxim Y. Balakirev
DOI:10.1021/ja204016e
日期:2011.7.6
Fluorescence imaging in clinical diagnostics and biomedical research relies to a great extent on the use of small organic fluorescent probes. Because of the difficulty of combining fluorescent and molecular-recognition properties, the development of such probes has been severely restricted to a number of well-known fluorescent scaffolds. Here we demonstrate that autofluorescing druglike molecules are a valuable source of bioimaging probes. Combinatorial synthesis and screening of chemical libraries in droplet microarrays allowed the identification of new types of fluorophores. Their concise and clean assembly by a multicomponent reaction presents a unique potential for the one-step synthesis of thousands of structurally diverse fluorescent molecules. Because they are based upon a druglike scaffold, these fluorophores retain their molecular recognition potential and can be used to design specific imaging probes.
Efficient Synthesis of 3-Aminoimidazo[1,2-a] Pyridines Using Silica-Supported Perchloric Acid (HClO4-SiO2) as a Novel Heterogenous Catalyst
作者:Azizollah Habibi、Zahra Tarameshloo、Shahnaz Rostamizadeh、Ali M. Amani
DOI:10.2174/157017812800167439
日期:2012.3.1
An efficient and green protocol for synthesis of 3-aminoimidazo[1,2-a] pyridine derivatives through a three-component reaction of aldehyde, 2-amino pyridine and isocyanide in the presence of silica-supportedperchloricacid (HClO4-SiO2) is described in this paper. The solid catalyst could be recycled and reused.