Bioorganic and Medicinal Chemistry Letters p. 1077 - 1082 (1998)
Update date:2022-08-02
Topics:
Patel, Mona
Kaltenbach III, Robert F.
Nugiel, David A.
McHugh Jr., Robert J.
Jadhav, Prabhakar K.
Bacheler, Lee T.
Cordova, Beverly C.
Klabe, Ronald M.
Erickson-Viitanen, Susan
Garber, Sena
Reid, Carol
Seitz, Steven P.
Cyclic urea SD 146, 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.
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(1961)