Abstract
(Chemical Equation Presented) No isolation, no purification. An efficient and simple method based on tetrabutylammonium fluoride-mediated alkylation without protecting groups in microtiter plates, followed by screening in situ has been developed to identify new enzyme inhibitors, as demonstrated in the discovery of the shown potent inhibitors of cathepsin B and HIV protease. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.