Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Bioorganic and Medicinal Chemistry

Volumn 26, Issue 8, 2018, Pages 1797-1809

  Sutherland, Hamish S ^a   Tong, Amy S T ^a   Choi, Peter J ^a   Conole, Daniel ^a   Blaser, Adrian ^a   Franzblau, Scott G ^c   Cooper, Christopher B ^d   Upton, Anna M ^d   Lotlikar, Manisha U ^d   Denny, William A ^a,b   Palmer, Brian D ^a,b  

^a UNIVERSITY OF AUCKLAND   (New Zealand)

^b UNIVERSITY OF AUCKLAND   (New Zealand)

^c UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

^d GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT   (United States)

Author keywords

Bedaquiline; Bedaquiline analogs; Drug development; Tuberculosis

Indexed keywords

BEDAQUILINE; BEDAQUILINE DERIVATIVE; NAPHTHALENE; POTASSIUM CHANNEL HERG; QUINOLINE DERIVATIVE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; FUSED HETEROCYCLIC RINGS; NAPHTHALENE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIUM CULTURE; CONTROLLED STUDY; CYTOTOXICITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; LIVER MICROSOME; MALE; MIC90; MOUSE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUBERCULOSIS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECT; MICROBIAL SENSITIVITY TEST; SYNTHESIS; TUMOR CELL LINE;

ANTITUBERCULAR AGENTS; BRIDGED BICYCLO COMPOUNDS, HETEROCYCLIC; CELL LINE, TUMOR; DIARYLQUINOLINES; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; MYCOBACTERIUM TUBERCULOSIS; NAPHTHALENES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85042370032     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2018.02.026     Document Type: Article

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