NOVEL CONFORMATIONALLY CONSTRAINED HIV-1 PROTEASE INHIBITORS - RATIONAL DESIGN, ENZYME-INHIBITION, AND X-RAY STRUCTURE OF AN ENZYME-INHIBITOR COMPLEX

A new class of conformationally restricted HIV-1 protease inhibitors w as designed based upon molecular modeling studies of known hydroxyethy lamine (HEA) type inhibitors. The structure activity relationships for this series of compounds are discussed and an X-ray crystal complex b etween one of the inhibitors, L-707,897 and HIV-1 protease is presente d.