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Computational Study of KNI-272, a Potent Inhibitor of HIV-1 Protease: On the Mechanism of Preorganization

✍ Scribed by David, Laurent; Luo, Ray; Head, Martha S.; Gilson, Michael K.


Book ID
126306482
Publisher
American Chemical Society
Year
1999
Tongue
English
Weight
281 KB
Volume
103
Category
Article
ISSN
0022-3654

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The effects of dose on the pharmacokinetic characteristics of KNI-272 were evaluated in rats after intravenous (iv) administration. The plasma kinetics of KNI-272 were dose-independent within a dose range of 1.0 to 10.0 mg/kg. However, when the dose was increased to 50.0 mg/kg, the area under the pl

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The binding characteristics of KNI-272, a potent and selective human immunodeficiency virus (HIV) protease inhibitor, were evaluated in rat and human plasma, and in solutions of human a,-acid glycoprotein (AAG) and human serum albumin (HSA). The unbound fractions (F,) of KNI-272 were 12.13 and 2.24%