Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 10, 2003, Pages 1821-1824

  Lu, Zhijian ^a   Raghavan, Subharekha ^a   Bohn, Joann ^a   Charest, Mark ^a   Stahlhut, Mark W ^a   Rutkowski, Carrie A ^a   Simcoe, Amy L ^a   Olsen, David B ^a   Schleif, William A ^a   Carella, Anthony ^a   Gabryelski, Lori ^a   Jin, Lixia ^a   Lin, Jiunn H ^a   Emini, Emilio ^a   Chapman, Kevin ^a   Tata, James R ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; CARBOXYLIC ACID DERIVATIVE; INDINAVIR; PROTEINASE INHIBITOR;

ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG DETERMINATION; DRUG EFFICACY; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYBRID; IC 50; LYMPHOID CELL; NONHUMAN; VIRUS RESISTANCE; VIRUS TYPING; WILD TYPE;

EID: 0038066624     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00262-2     Document Type: Article

References (14)

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13. 3, 500 MHz): 1:1 mixture of rotamers: 6.80-7.70 (m, 12H), 6.00 (m, 2H), 5.18 (m, 1H), 4.85 (m, 3H), 4.70 (s, 1/2H), 4.61 (m, 1H), 4.40 (s, 1/2H), 4.38 (m, 1H), 4.05 (m, 3H), 3.78 (m, 1H), 2.80-3.10 (m, 4H), 2.20 (m, 1H), 1.61 (m, 1H), 1.60 (s, 3/2H), 1.57 (s, 3/2H), 1.40 (s, 3/2H), 1.39 (s, 3/2H). LC-MS (ES) 686.1 (M+1).
14. 3, 500 MHz): 1:1 mixture of rotamers: 6.80-7.40 (m, 9H), 5.88 (br.S, 1H), 5.10 (m, 1H), 4.90 (m, 1H), 4.65 (s, 1/2H), 4.40 (3/2H), 4.29 (m, 1H), 4.05 (m, 2H), 3.72 (m, 1H), 2.88 (m, 4H), 2.53 (s, 3/2H), 2.50 (s, 3/2H), 2.40 (s, 3H), 2.08 (m, 1H), 1.59 (s, 3/2H), 1.56 (s, 3/2H), 1.42 (s, 3/2H), 1.36 (s, 3/2H). LC-MS (ES) 653.1 (M+1).