Optimization of small molecule drugs binding to highly polar target sites: Lessons from the discovery and development of neuraminidase inhibitors

Current Topics in Medicinal Chemistry

Volumn 6, Issue 5, 2006, Pages 423-434

  Klumpp, Klaus ^a   Graves, Bradford J ^b  

^a ROCHE BIOSCIENCE   (United States)

^b HOFFMANN LA ROCHE INC   (United States)

Author keywords

Antiviral agents; Antiviral therapy; Lead optimization; Neuraminidase

Indexed keywords

4 ACETAMIDO 5 AMINO 3 (1 ETHYLPROPOXY) 1 CYCLOHEXENE 1 CARBOXYLIC ACID; ABT 675; ANTIVIRUS AGENT; GLYCOPROTEIN; N ACETYL 2,3 DIDEHYDRO 2 DEOXYNEURAMINIC ACID; OSELTAMIVIR; PERAMIVIR; SIALIC ACID; SIALIDASE; SIALIDASE INHIBITOR; UNCLASSIFIED DRUG; ZANAMIVIR;

BINDING AFFINITY; DRUG BIOAVAILABILITY; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG RESEARCH; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME MECHANISM; HUMAN; INFLUENZA; MOLECULAR INTERACTION; NONHUMAN; REVIEW;

ACETAMIDES; ANIMALS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; INFLUENZA, HUMAN; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR WEIGHT; NEURAMINIDASE; OSELTAMIVIR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33646124511     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802606776743138     Document Type: Review

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