EXPEDIENT METHOD FOR THE SOLID-PHASE SYNTHESIS OF ASPARTIC-ACID PROTEASE INHIBITORS DIRECTED TOWARD THE GENERATION OF LIBRARIES

Dunn B.M., Structure and Function of the Aspartic Proteinoses, (1991)

Greenlee W.J., Renin Inhibitors, Med. Res. Rev., 10, pp. 173-236, (1990)

Wiley R.A., Rich D.H., Peptidomimetics Derived from Natural Products, Med. Res. Rev., 13, pp. 327-384, (1993)

Baldwin E.T., Bhat T.N., Gulnik S., Hosur M.V., Sowder R.C., Cachau R.E., Collins J., Silva A.M., Erickson J.W., Crystal Structures of Native and Inhibited Forms of Human Cathepsin D: Implication for Lysosomal Targeting and Drug Design, Proc. Natl. Acad. Sci. U. SA., 90, pp. 6796-6800, (1993)

Roberts N.A., Martin J.A., Kinchington D., Broadhurst A.V., Craig J.C., Duncan I.B., Galpin S.A., Handa B.K., Kay J., Krohn A., Lambert R.W., Merrett J.H., Mills J.S., Parkes K.E.B., Redshaw S., Ritchie A.J., Taylor D.L., Thomas G.J., Machin P.J., Rational Design of Peptide-Based HIV Proteinase Inhibitors, Science, 248, pp. 358-361, (1990)

Getman D.P., DeCrescenzo G.A., Heintz R.M., Reed K.L., Talley J.J., Bryant M.L., Clare M., Houseman K.A., Marr J.J., Mueller R.A., Vazquez M.L., Shieh H.-S., Stallings W.C., Stegeman R.A., Discovery of a Novel Class of Potent HIV-1 Protease Inhibitors Containing the (R)-(Hydroxyethyl) urea Isostere, J. Med. Chem., 36, pp. 288-291, (1993)

Kim B.M., Vacca J.P., Guare J.P., Hanifin C.M., Michelson S.R., Darke P.L., Zugay J.A., Emini E.A., Schleif W., Lin J.H., Chen I.-W., Vastag K., Ostovic D., Anderson P.S., Huff J.R., A New Hydroxyethy- lamine Class of HIV-1 Protease Inhibitors with High Antiviral Potency and Oral Bioavailability, BioMed. Chem. Lett., 4, pp. 2273-2278, (1994)

Kim E.E., Baker C.T., Dwyer M.D., Murcko M.A., Rao B.G., Tung R.D., Navia M.A., Crystal Structure of HIV-1 Protease in Complex with VX-478, a Potent and Orally Bioavailable Inhibitor of the Enzyme, J. Am. Chem. Soc., 117, pp. 1181-1182, (1995)

Smith A.B., Hirschmann R., Pasternak A., Akaishi R., Guzman M.C., Jones D.R., Keenan T.P., Sprengeler P.A., Darke P.L., Emini E.A., Holloway M.K., Schleif W.A., Design and Synthesis of Peptidomimetic Inhibitors of HIV-1 Protease and Renin. Evidence for Improved Transport, J. Med. Chem., 37, pp. 215-218, (1994)

Lam P.Y.S., Jadhav P.K., Eyermann C.J., Hodge C.N., Ru Y., Bacheler L.T., Meek J.L., Otto M.J., Rayner M.M., Wong Y.N., Chang C.-H., Weber P.C., Jackson D.A., Sharpe T.R., Erickson-Viitanen S., Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors, Science, 263, pp. 380-384, (1994)

Dunn B.M., Structure and Function of the Aspartic Proteinoses, (1991)

Greenlee W.J., Renin Inhibitors, Med. Res. Rev., 10, pp. 173-236, (1990)

Wiley R.A., Rich D.H., Peptidomimetics Derived from Natural Products, Med. Res. Rev., 13, pp. 327-384, (1993)

Baldwin E.T., Bhat T.N., Gulnik S., Hosur M.V., Sowder R.C., Cachau R.E., Collins J., Silva A.M., Erickson J.W., Crystal Structures of Native and Inhibited Forms of Human Cathepsin D: Implication for Lysosomal Targeting and Drug Design, Proc. Natl. Acad. Sci. U. SA., 90, pp. 6796-6800, (1993)

Roberts N.A., Martin J.A., Kinchington D., Broadhurst A.V., Craig J.C., Duncan I.B., Galpin S.A., Handa B.K., Kay J., Krohn A., Lambert R.W., Merrett J.H., Mills J.S., Parkes K.E.B., Redshaw S., Ritchie A.J., Taylor D.L., Thomas G.J., Machin P.J., Rational Design of Peptide-Based HIV Proteinase Inhibitors, Science, 248, pp. 358-361, (1990)

Getman D.P., DeCrescenzo G.A., Heintz R.M., Reed K.L., Talley J.J., Bryant M.L., Clare M., Houseman K.A., Marr J.J., Mueller R.A., Vazquez M.L., Shieh H.-S., Stallings W.C., Stegeman R.A., Discovery of a Novel Class of Potent HIV-1 Protease Inhibitors Containing the (R)-(Hydroxyethyl) urea Isostere, J. Med. Chem., 36, pp. 288-291, (1993)

Kim B.M., Vacca J.P., Guare J.P., Hanifin C.M., Michelson S.R., Darke P.L., Zugay J.A., Emini E.A., Schleif W., Lin J.H., Chen I.-W., Vastag K., Ostovic D., Anderson P.S., Huff J.R., A New Hydroxyethy- lamine Class of HIV-1 Protease Inhibitors with High Antiviral Potency and Oral Bioavailability, BioMed. Chem. Lett., 4, pp. 2273-2278, (1994)

Kim E.E., Baker C.T., Dwyer M.D., Murcko M.A., Rao B.G., Tung R.D., Navia M.A., Crystal Structure of HIV-1 Protease in Complex with VX-478, a Potent and Orally Bioavailable Inhibitor of the Enzyme, J. Am. Chem. Soc., 117, pp. 1181-1182, (1995)

Smith A.B., Hirschmann R., Pasternak A., Akaishi R., Guzman M.C., Jones D.R., Keenan T.P., Sprengeler P.A., Darke P.L., Emini E.A., Holloway M.K., Schleif W.A., Design and Synthesis of Peptidomimetic Inhibitors of HIV-1 Protease and Renin. Evidence for Improved Transport, J. Med. Chem., 37, pp. 215-218, (1994)

Lam P.Y.S., Jadhav P.K., Eyermann C.J., Hodge C.N., Ru Y., Bacheler L.T., Meek J.L., Otto M.J., Rayner M.M., Wong Y.N., Chang C.-H., Weber P.C., Jackson D.A., Sharpe T.R., Erickson-Viitanen S., Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors, Science, 263, pp. 380-384, (1994)