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37. Kaldor SW, Appelt K, Fritz JE, Hammond M, Crowell TA, Baxter AJ, Hatch SD, Wiskerchen MA,
Muesing MA. A systemic study of P1–P3 spanning sidechains for the inhibition of HIV-1 protease.
Bioorg. Med. Chem. Lett. 1995; 5:715–720.
38. Kalish JV, Tatlock JH, Davies JF, Kaldor SW, Dressman BA, Reich S, Pino M, Nyugen D, Appelt
K, Musick L, Wu B-W. Structure-based drug design of nonpeptidic P2 substituents for HIV-1 protease
inhibitors. Bioorg. Med. Chem. Lett. 1995; 5:727–732.
39. Kaldor SW, Kalish VJ, Davies JF, Appelt K, Tatlock JH, Dressman BA, Campanale KM, Burgess
JA, Lubbehusen PL, Muesing MA, Hatch SD, Shetty BV, Patick AK, Kosa MB, Khalil DA. AG1343: a
potent orally bioavailable inhibitor of HIV-1 protease. J. Med. Chem. 1996; submitted for publication.
40. Shetty B, Kosa M, Khalil DA, Webber S. Preclinical Pharmacokinetics and Distribution to Tissue of
AG1343, an inhibitor of human deficiency virus type 1 protease. Antimicr. Ag. and Chemoth. 1996;
40:110–114.
41. Quart BD, Chapman SK, Peterkin J, Webber S, Oliver S. Phase 1 safety, tolerance,
pharmacokinetics and food effect studies of AG1343—a novel HIV protease inhibitor. Abst. LB3. In:
Proceedings of the 2nd National Conference on Human Retroviruses and Related Infections. 1995:163.
42. Lam PYS, Jadhaw PK, Eyermann CJ, Hodge CN, Lee YR, Bacheler LT, Meek JL, Otto MJ, Rayner
MM, Wong YN, Chang C-H, Weber PC, Jackson DA, Sharpe TR, Erickson-Viitanen S. Rational design
of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors. Science, 1994; 263:380–384.
43. Reich SH, Melnick M, Davies JF, Appelt K, Lewis KK, Fuhry MA, Pino M, Trippe AJ, Nguyen D,
Dawson H, Wu B-W, Musick L, Kosa M, Kahil D, Webber S, Gehlhaar DK, Andrada D, Shetty B.
Protein structure-based design of potent, orally bioavailable, nonpeptide inhibitors of human
immunodeficiency virus protease. Proc. Natl. Acad. Sci. 1995; 92:3298–3302.
44. Reich SH, Melnick M, Pino M, Fuhry MA, Trippe AJ, Appelt K, Davies JF, Wu B-W, Musick L.
Structure-based design and synthesis of substituted 2-butanols as nonpeptidic inhibitors of HIV protease:
secondary amide series. J. Med. Chem. 1996; 39:2781–2794.
45. Melnick M, Reich SH, Lewis KK, Mitchell L, Ngyen D, Trippe AJ, Dawson H, Davies JF, Appelt
K, Wu B-W, Musick L, Gehlhaar DK, Webber S, Shetty B, Kosa M, Kahil D, Andrada D. Bis-tertiary
amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design. J. Med.
Chem. 1996; 39:2795–2811.
46. Gehlhaar DK, Moerder KE, Zichi D, Sherman CJ, Ogden RC, Freer ST. De novo design of enzyme
inhibitors by Monte Carlo ligand generation. J. Med. Chem. 1995; 38:466–472.
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