Diversity-oriented synthesis probe targets plasmodium falciparum cytochrome b ubiquinone reduction site and synergizes with oxidation site inhibitors

Journal of Infectious Diseases

Volumn 211, Issue 7, 2015, Pages 1097-1103

  Lukens, Amanda K ^a,b   Heidebrecht, Richard W ^a   Mulrooney, Carol ^c   Beaudoin, Jennifer A ^c   Comer, Eamon ^c   Duvall, Jeremy R ^c   Fitzgerald, Mark E ^c   Masi, Daniela ^c   Galinsky, Kevin ^d   Scherer, Christina A ^c   Palmer, Michelle ^c   Munoz, Benito ^c   Foley, Michael ^c   Schreiber, Stuart L ^a   Wiegand, Roger C ^a   Wirth, Dyann F ^a,b  

^a BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^b HARVARD SCHOOL OF PUBLIC HEALTH   (United States)

^c Therapeutics Platform   (United States)

^d Genome Sequence and Analysis Program   (United States)

Author keywords

cytochrome b; diversity oriented synthesis; drug development; drug resistance; malaria; target identification

Indexed keywords

ANTIMALARIAL AGENT; CHLOROQUINE; CITRININ; CYTOCHROME B; ML 238; N [[11 [1 (DIMETHYLAMINO)PROPAN 2 YL] 14 [3 (3,5 DIMETHYLISOXAZOL 4 YL)UREIDO] 2,9 DIMETHYL 12 OXO 2,3,4,5,6,8,9,10,11,12 DECAHYDROBENZO [B][1,9,5]DIOXAAZACYCLOTETRADECIN 8 YL]METHYL] 4 FLUORO N METHYLBENZENESULFONAMIDE; UNCLASSIFIED DRUG; CARBANILAMIDE DERIVATIVE; ENZYME INHIBITOR; MACROCYCLIC LACTAM; ML238 COMPOUND; MOLECULAR LIBRARY; N-((11-(1-(DIMETHYLAMINO)PROPAN-2-YL)-14-(3-(3,5-DIMETHYLISOXAZOL-4-YL)UREIDO)-2,9-DIMETHYL-12-OXO-2,3,4,5,6,8,9,10,11,12-DECAHYDROBENZO(B)(1,9,5)DIOXAAZACYCLOTETRADECIN-8-YL)METHYL)-4-FLUORO-N-METHYLBENZENESULFONAMIDE; PROTOZOAL PROTEIN; UBIQUINONE;

CONFERENCE PAPER; CONTROLLED STUDY; DIVERSITY ORIENTED SYNTHESIS; DRUG POTENTIATION; DRUG RESISTANCE; DRUG SCREENING; DRUG SYNTHESIS; EC50; GENE SEQUENCE; MALARIA; NONHUMAN; NUCLEOTIDE SEQUENCE; OXIDATION; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; PROTEIN TARGETING; REDUCTION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYME ACTIVE SITE; ENZYMOLOGY; GENETICS; HIGH THROUGHPUT SCREENING; HIGH THROUGHPUT SEQUENCING; HUMAN; MALARIA, FALCIPARUM; METABOLISM; MOLECULAR GENETICS; MOLECULAR LIBRARY; OXIDATION REDUCTION REACTION; PARASITOLOGY; PROCEDURES; SYNTHESIS;

ANTIMALARIALS; BASE SEQUENCE; CATALYTIC DOMAIN; CYTOCHROMES B; DRUG DISCOVERY; DRUG RESISTANCE; DRUG SYNERGISM; ENZYME INHIBITORS; HIGH-THROUGHPUT NUCLEOTIDE SEQUENCING; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LACTAMS, MACROCYCLIC; MALARIA, FALCIPARUM; MOLECULAR SEQUENCE DATA; OXIDATION-REDUCTION; PHENYLUREA COMPOUNDS; PLASMODIUM FALCIPARUM; PROTOZOAN PROTEINS; SMALL MOLECULE LIBRARIES; UBIQUINONE;

EID: 84927729717     PISSN: 00221899     EISSN: 15376613     Source Type: Journal    
DOI: 10.1093/infdis/jiu565     Document Type: Conference Paper

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