Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: The present invention provides methods of screening for ligands of target molecules. The methods of the present invention include assays in which a target molecule is subjected to denaturing conditions, and compounds are screened for the ability to alter the susceptibility of the target to unfolding. The methods of the present invention use fluorescence detection to determine that degree of unfolding of a target molecule. In some aspects of the present invention, fluorescence resonance energy transfer (FRET) is detected. In other aspects of the invention, fluorescence polarization (FP) is detected. In preferred embodiments, a target molecule such as a target protein is heated to a temperature, called TATLAS, at which at least a portion of the target molecule unfolds, in the presence of a test compound.