Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity

Journal of Medicinal Chemistry

Volumn 56, Issue 21, 2013, Pages 8860-8871

  Younis, Yassir ^a   Douelle, Frederic ^a   González Cabrera, Diego ^a   Le Manach, Claire ^a   Nchinda, Aloysius T ^a   Paquet, Tanya ^a   Street, Leslie J ^a   White, Karen L ^b   Zabiulla, K Mohammed ^c   Joseph, Jayan T ^c   Bashyam, Sridevi ^c   Waterson, David ^d   Witty, Michael J ^d   Wittlin, Sergio ^e,f   Charman, Susan A ^b   Chibale, Kelly ^a  

^a UNIVERSITY OF CAPE TOWN   (South Africa)

^b MONASH UNIVERSITY   (Australia)

^c SYNGENE INTERNATIONAL LTD   (India)

^d Medicines for Malaria Venture   (Switzerland)

^e SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^f UNIVERSITY OF BASEL   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

(4 (5 AMINO 6 (4 (TRIFLUOROMETHYL)PHENYL)PYRAZIN 2YL)PHENYL) (MORPHOLINO)METHANONE; 2 AMINOPYRIDINE DERIVATIVE; 4 (5 AMINO 6 (6 (TRIFLUOROMETHYL)PYRIDIN 3 YL)PYRAZIN 2 YL) N METHYLBENZENESULFONAMIDE; 5 (4 (ETHYLSULFONYL)PHENYL) 3 (6 (TRIFLUOROMETHYL)PYRIDIN 3 YL)PYRAZIN 2 AMINE; 5 (4 (METHYLSULFONYL)PHENYL) 3 (4 (TRIFLUOROMETHYL)PHENYL)PYRAZIN 2 AMINE; 5 (4 METHYLSULFONYL)PHENYL) 3 (6 (TRIFLUOROMETHYL)PYRIDIN 3 YL)PYRAZIN 2 AMINE; ANTIMALARIAL AGENT; ARTESUNATE; CHLOROQUINE; POTASSIUM CHANNEL HERG; PYRIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; ARTICLE; CROSS COUPLING REACTION; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG SAFETY; DRUG SOLUBILITY; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; LIVER CLEARANCE; LIVER MICROSOME; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; PLASMODIUM BERGHEI INFECTION; PLASMODIUM FALCIPARUM; STRUCTURE ACTIVITY RELATION; SURVIVAL TIME; SUZUKI REACTION;

ADMINISTRATION, ORAL; AMINOPYRIDINES; ANIMALS; ANTIMALARIALS; CHO CELLS; CRICETULUS; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MICE; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PARASITIC SENSITIVITY TESTS; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84887883886     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401278d     Document Type: Article

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