Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

Journal of Medicinal Chemistry

Volumn 57, Issue 17, 2014, Pages 7465-7471

  Bruno, Stefano ^a,d   Pinto, Andrea ^b   Paredi, Gianluca ^a   Tamborini, Lucia ^b   De Micheli, Carlo ^b   La Pietra, Valeria ^c   Marinelli, Luciana ^c   Novellino, Ettore ^c   Conti, Paola ^b   Mozzarelli, Andrea ^a,e  

^a UNIVERSITY OF PARMA   (Italy)

^b UNIVERSITY OF MILAN   (Italy)

^c UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^d CNR   (Italy)

^e NATIONAL INSTITUTE OF BIOSTRUCTURES AND BIOSYSTEMS   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

3 BROMO 5 (PYRIDIN 4 YL) 4,5 DIHYDROISOXAZOLE; 3 BROMO 5 PHENYL 4,5 DIHYDROISOXAZOLE; 3 BROMO ISOXAZOLINE DERIVATIVE; 3 CHLORO 5 5 PHENYL 4,5 DIHYDROISOXAZOLE; 4 (3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)PHENOL; ANTIMALARIAL AGENT; BENZYL 2 (3 BROMO 4,5 DIHYDROISOXAZOL 5 YL) 2 (TERT BUTOXYCARBONYLAMINO)ACETATE; BENZYL 2 AMINO 2 (3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)ACETATE; CYSTEINE; GLYCERALDEHYDE 3 PHOSPHATE DEHYDROGENASE; GLYCERALDEHYDE 3 PHOSPHATE DEHYDROGENASE INHIBITOR; ISOXAZOLINE DERIVATIVE; METHYL 2 (3 BROMO 4,5 DIHYDROISOXAZOL 5 YL) 2 (TERT BUTOXYCARBONYLAMINO)ACETATE; METHYL 2 AMINO 2 ( 3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)ACETATE; UNCLASSIFIED DRUG; ENZYME INHIBITOR; ISOXAZOLE DERIVATIVE; MOLECULAR LIBRARY; PROTEIN BINDING; PROTOZOAL PROTEIN;

ABSORPTION SPECTROSCOPY; ARTICLE; CATALYSIS; CYCLOADDITION; DRUG SYNTHESIS; ENZYME INHIBITION; MALARIA; MASS SPECTROMETRY; MATRIX ASSISTED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOCATALYSIS; CHEMICAL MODEL; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; HUMAN; KINETICS; MALARIA, FALCIPARUM; METABOLISM; MOLECULAR LIBRARY; PARASITOLOGY; PHARMACOLOGY; PHYSIOLOGY; PLASMODIUM FALCIPARUM; PROTEIN TERTIARY STRUCTURE; SPECTROPHOTOMETRY; STATIC ELECTRICITY; SYNTHESIS; TIME;

ANIMALS; BIOCATALYSIS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME INHIBITORS; GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASES; HUMANS; ISOXAZOLES; KINETICS; MALARIA, FALCIPARUM; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PLASMODIUM FALCIPARUM; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTOZOAN PROTEINS; SMALL MOLECULE LIBRARIES; SPECTROMETRY, MASS, MATRIX-ASSISTED LASER DESORPTION-IONIZATION; SPECTROPHOTOMETRY; STATIC ELECTRICITY; TIME FACTORS;

EID: 84907185154     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500747h     Document Type: Article

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