Design and optimization of highly-selective fungal CYP51 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 15, 2014, Pages 3455-3458

  Hoekstra, William J ^a   Garvey, Edward P ^a   Moore, William R ^a   Rafferty, Stephen W ^a   Yates, Christopher M ^a   Schotzinger, Robert J ^a  

^a Viamet Pharmaceuticals   (United States)

Author keywords

Azole; CYP51; Fungal infection; Lanosterol demethylase

Indexed keywords

ANTIFUNGAL AGENT; CYTOCHROME P450 3A4; ITRACONAZOLE; POSACONAZOLE; STEROL 14ALPHA DEMETHYLASE; STEROL 14ALPHA DEMETHYLASE INHIBITOR; UNCLASSIFIED DRUG; VORICONAZOLE; VT 1161; CYTOCHROME P450 2C19; FUNGAL ENZYME; MOLECULAR SCAFFOLD; PYRIMIDINE DERIVATIVE; TRIAZOLE DERIVATIVE;

ANTIFUNGAL ACTIVITY; ARTICLE; CANDIDA ALBICANS; CHEMICAL MODIFICATION; DERMATOPHYTE; DRUG DESIGN; FUNGAL STRAIN; IC 50; IN VITRO STUDY; METAL BINDING; MYCOSIS; PHASE 2 CLINICAL TRIAL (TOPIC); PHYSICAL CHEMISTRY; PROTEIN TARGETING; TRICHOPHYTON RUBRUM; BINDING AFFINITY; CONTROLLED STUDY; DRUG POTENCY; DRUG TARGETING; ENZYME ACTIVE SITE; FUNGUS GROWTH; HUMAN; HUMAN CELL; IC50; MICROSOME; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; CHEMISTRY; CONFORMATION; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; GROWTH, DEVELOPMENT AND AGING; METABOLISM; MICROBIAL SENSITIVITY TEST; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

14-ALPHA DEMETHYLASE INHIBITORS; ANTIFUNGAL AGENTS; CANDIDA ALBICANS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; MICROBIAL SENSITIVITY TESTS; MOLECULAR CONFORMATION; STEROL 14-DEMETHYLASE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84904044317     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.05.068     Document Type: Article

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