Symmetric fluoro-substituted diol-based HIV protease inhibitors: Ortho-fluorinated and meta-fluorinated P1/P1′-benzyloxy side groups significantly improve the antiviral activity and preserve binding efficacy

European Journal of Biochemistry

Volumn 271, Issue 22, 2004, Pages 4594-4602

  Lindberg, Jimmy ^a   Pyring, David ^b   Löwgren, Seved ^a   Rosenquist, Åsa ^b   Zuccarello, Guido ^b   Kvarnström, Ingemar ^b   Zhang, Hong ^c   Vrang, Lotta ^c   Classon, Björn ^c,d   Hallberg, Anders ^a   Samuelsson, Bertil ^c,d   Unge, Torsten ^a  

^a UPPSALA UNIVERSITY   (Sweden)

^b LINKÖPING UNIVERSITY   (Sweden)

^c MEDIVIR AB   (Sweden)

^d STOCKHOLM UNIVERSITY   (Sweden)

Author keywords

AIDS; Aspartic protease; Crystal structure; Fluorine; HIV

Indexed keywords

ASPARTIC PROTEINASE; INDANOLEAMINE; INDANONE DERIVATIVE; INDINAVIR; NELFINAVIR; PROTEINASE; PROTEINASE INHIBITOR; RITONAVIR; SAQUINAVIR; UNCLASSIFIED DRUG;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIVIRAL ACTIVITY; ARTICLE; CRYSTAL STRUCTURE; DRUG STRUCTURE; ENZYME INHIBITION; FLUORINATION; HUMAN IMMUNODEFICIENCY VIRUS; LIFE CYCLE; PHARMACOKINETICS; PRIORITY JOURNAL; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION; VIRION; VIRUS; VIRUS PARTICLE; X RAY CRYSTALLOGRAPHY;

AMINO ACIDS; BENZENE DERIVATIVES; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; ELECTROSTATICS; ESCHERICHIA COLI; HIV PROTEASE; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; HYDROCARBONS, FLUORINATED; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; PROTEIN BINDING; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 9644295843     PISSN: 00142956     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1432-1033.2004.04431.x     Document Type: Article

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