The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.

Abstract

Cyclic urea SD146, a potent HIV protease inhibitor bearing a flat resistance profile, possessed poor solubility and bioavailability, which precluded further development of the compound. In an effort to improve upon the pharmacokinetic profile of the compound, several analogs modified at the P1/P1' residues were prepared and evaluated. Several of those compounds displayed significant improvement of physical properties.

Cite this paper

@article{Patel1998TheSO, title={The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.}, author={Mahesh G. Patel and Robert F Kaltenbach and David A Nugiel and Robert J McHugh and Prabhakar K. Jadhav and Lee Bacheler and Beverly C Cordova and Ronald M. Klabe and Susan K Erickson-Viitanen and Salome Garber and Carrolyn S Reid and Steven P. Seitz}, journal={Bioorganic & medicinal chemistry letters}, year={1998}, volume={8 9}, pages={1077-82} }