Synthesis, antiviral activity and pharmacokinetics of P1/P1′ substituted 3-aminoindazole cyclic urea HIV protease inhibitors

Robert F Kaltenbach,Mona Patel,Robert E Waltermire,Gregory D Harris,Benjamin R.P Stone,Ronald M Klabe,Sena Garber,Lee T Bacheler,Beverly C Cordova,Kelly Logue,Matthew R Wright,Susan Erickson-Viitanen,George L Trainor

Bioorganic & Medicinal Chemistry Letters（2003）

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摘要

A series of P1/P1′ substituted cyclic urea analogues were prepared in an attempt to increase the intra-cellular antiviral potency of the nonsymmetrical 3-aminoindazoles DMP 850 and DMP 851. The effect of alkyl substitution of the P1/P1′ residues on cellular antiviral potency, protein binding, resistance profile and pharmacokinetics are described.

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protein binding

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