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

Abstract 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.