Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): Cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities

Journal of Medicinal Chemistry

Volumn 58, Issue 7, 2015, Pages 3117-3130

  Witschel, Matthias C ^a   Rottmann, Matthias ^b,c   Schwab, Anatol ^d   Leartsakulpanich, Ubolsree ^e   Chitnumsub, Penchit ^e   Seet, Michael ^d   Tonazzi, Sandro ^d   Schwertz, Geoffrey ^d   Stelzer, Frank ^a   Mietzner, Thomas ^a   McNamara, Case ^f   Thater, Frank ^a   Freymond, Céline ^b,c   Jaruwat, Aritsara ^e   Pinthong, Chatchadaporn ^g   Riangrungroj, Pinpunya ^e   Oufir, Mouhssin ^c   Hamburger, Matthias ^c   Mäser, Pascal ^b,c   Sanz Alonso, Laura M ^h   Charman, Susan ⁱ   Wittlin, Sergio ^b,c   Yuthavong, Yongyuth ^e   Chaiyen, Pimchai ^g   Diederich, François ^d   more..

^a BASF SE   (Germany)

^b SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^c UNIVERSITY OF BASEL   (Switzerland)

^d ETH ZURICH   (Switzerland)

^e NATIONAL SCIENCE AND TECHNOLOGY DEVELOPMENT AGENCY   (Thailand)

^f California Institute for Biomedical Research   (United States)

^g MAHIDOL UNIVERSITY   (Thailand)

^h GLAXOSMITHKLINE   (Spain)

ⁱ MONASH UNIVERSITY   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; GLYCINE HYDROXYMETHYLTRANSFERASE; PYRAN DERIVATIVE; PYRAZOLE DERIVATIVE; PYRAZOLOPYRAN DERIVATIVE; UNCLASSIFIED DRUG; ENZYME INHIBITOR; PYRAZOLE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; MAMMAL CELL; MOUSE; NONHUMAN; PLASMODIUM BERGHEI; PLASMODIUM BERGHEI INFECTION; PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; DRUG RESISTANCE; DRUG SCREENING; ENZYMOLOGY; FEMALE; HEPG2 CELL LINE; INBRED MOUSE STRAIN; LIVER; LIVER MICROSOME; MALARIA, FALCIPARUM; METABOLISM; ORAL DRUG ADMINISTRATION; PARASITOLOGY; PATHOGENICITY; PROCEDURES; RAT; SCID MOUSE; SYNTHESIS; TRANSGENIC ORGANISM; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; ANTIMALARIALS; CHEMISTRY TECHNIQUES, SYNTHETIC; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE; ENZYME INHIBITORS; FEMALE; GLYCINE HYDROXYMETHYLTRANSFERASE; HEP G2 CELLS; HUMANS; LIVER; MALARIA, FALCIPARUM; MICE, INBRED STRAINS; MICE, SCID; MICROSOMES, LIVER; ORGANISMS, GENETICALLY MODIFIED; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PYRAZOLES; RATS;

EID: 84927603340     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501987h     Document Type: Article

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