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Chemical Compound Review:

aminoindazole 1H-indazol-3-amine

Synonyms: Amino-indazole, PubChem11848, SureCN18878, AG-F-48692, AG-H-52668, ...

Rodgers, J.D. et al., Rodgers, J.D. et al., Kaltenbach, R.F. et al., Garg, R. et al.

Kaltenbach, Patel, Waltermire, Harris, Stone, Klabe, Garber, Bacheler, Cordova, Logue, Wright, Erickson-Viitanen, Trainor, Rodgers, Lam, Johnson, Wang, Li, Ru, Ko, Seitz, Trainor, Anderson, Klabe, Bacheler, Cordova, Garber, Reid, Wright, Chang, Erickson-Viitanen, Garg, Bhhatarai,

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Disease relevance of NSC44677

RESULTS: We have discovered that nonsymmetrical cyclic ureas containing a 3-aminoindazole P2 group are potent inhibitors of HIV protease with excellent oral bioavailability [1].
A mechanistic study of 3-aminoindazole cyclic urea HIV-1 protease inhibitors using comparative QSAR [2].

High impact information on NSC44677

Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors [3].
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups [4].
The parent 3-aminoindazole 6 showed a Ki < 0.01 nM but poor translation of enzyme activity to antiviral activity was observed [4].

References

Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors. Rodgers, J.D., Lam, P.Y., Johnson, B.L., Wang, H., Li, R., Ru, Y., Ko, S.S., Seitz, S.P., Trainor, G.L., Anderson, P.S., Klabe, R.M., Bacheler, L.T., Cordova, B., Garber, S., Reid, C., Wright, M.R., Chang, C.H., Erickson-Viitanen, S. Chem. Biol. (1998) [Pubmed]
A mechanistic study of 3-aminoindazole cyclic urea HIV-1 protease inhibitors using comparative QSAR. Garg, R., Bhhatarai, B. Bioorg. Med. Chem. (2004) [Pubmed]
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors. Kaltenbach, R.F., Patel, M., Waltermire, R.E., Harris, G.D., Stone, B.R., Klabe, R.M., Garber, S., Bacheler, L.T., Cordova, B.C., Logue, K., Wright, M.R., Erickson-Viitanen, S., Trainor, G.L. Bioorg. Med. Chem. Lett. (2003) [Pubmed]
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups. Rodgers, J.D., Johnson, B.L., Wang, H., Erickson-Viitanen, S., Klabe, R.M., Bacheler, L., Cordova, B.C., Chang, C.H. Bioorg. Med. Chem. Lett. (1998) [Pubmed]

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