Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N -myristoyltransferase inhibitors: Identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human african trypanosomiasis

Journal of Medicinal Chemistry

Volumn 57, Issue 23, 2014, Pages 9855-9869

  Brand, Stephen ^a   Norcross, Neil R ^a   Thompson, Stephen ^a   Harrison, Justin R ^a   Smith, Victoria C ^a   Robinson, David A ^a   Torrie, Leah S ^a   McElroy, Stuart P ^a   Hallyburton, Irene ^a   Norval, Suzanne ^a   Scullion, Paul ^a   Stojanovski, Laste ^a   Simeons, Frederick R C ^a   Van Aalten, Daan ^a   Frearson, Julie A ^a   Brenk, Ruth ^a   Fairlamb, Alan H ^a   Ferguson, Michael A J ^a   Wyatt, Paul G ^a   Gilbert, Ian H ^a   Read, Kevin D ^a   more..

^a UNIVERSITY OF DUNDEE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2,6 DICHLORO 4 (2 PIPERAZIN 1 YL PYRIDIN 4 YL) N (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL) BENZENESULFONAMIDE; 2,6 DICHLORO N (DIFLUOROMETHYL) 4 [3 (1 METHYLPIPERIDIN 4 YL)PROPYL] N (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL)BENZENESULFONAMIDE; 4 BROMO 2,6 DICHLORO N (DIFLUOROMETHYL) N (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL)BENZENESULFONAMIDE; 4 BROMO N (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL) BENZENESULFONAMIDE; 4 BROMO N METHYL N (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL)BENZENESULFONAMIDE; ANTIPROTOZOAL AGENT; HYDROGEN; METHYL GROUP; PROTEIN N MYRISTOYLTRANSFERASE INHIBITOR; PYRAZOLE DERIVATIVE; SULFONAMIDE; UNCLASSIFIED DRUG; 2,6-DICHLORO-N-(DIFLUOROMETHYL)-4-(3-(1-METHYLPIPERIDIN-4-YL)PROPYL)-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE; ACYLTRANSFERASE; AMINOPYRIDINE DERIVATIVE; ANTITRYPANOSOMAL AGENT; DDD 85646; GLYCYLPEPTIDE N-TETRADECANOYLTRANSFERASE;

AFRICAN TRYPANOSOMIASIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG PENETRATION; DRUG POTENCY; DRUG SCREENING; EC50; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; LEISHMANIA MAJOR; MALE; MEMBRANE PERMEABILITY; METHYLATION; MOUSE; NONHUMAN; PH; PROCESS OPTIMIZATION; RAT; SONOGASHIRA REACTION; STRUCTURE ACTIVITY RELATION; SURFACE PROPERTY; SUZUKI REACTION; TRYPANOSOMA BRUCEI; ANIMAL; ANTAGONISTS AND INHIBITORS; CENTRAL NERVOUS SYSTEM; CHEMISTRY; DRUG EFFECTS; SYNTHESIS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMIASIS, AFRICAN;

ACYLTRANSFERASES; AMINOPYRIDINES; ANIMALS; BLOOD-BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; FEMALE; HUMANS; INHIBITORY CONCENTRATION 50; MICE; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMIASIS, AFRICAN;

EID: 84918563084     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500809c     Document Type: Article

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