Catechol pyrazolinones as trypanocidals: Fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1

Journal of Medicinal Chemistry

Volumn 55, Issue 20, 2012, Pages 8745-8756

  Orrling, Kristina M ^a   Jansen, Chimed ^a   Vu, Xuan Lan ^b   Balmer, Vreni ^b   Bregy, Patrick ^b,h   Shanmugham, Anitha ^c   England, Paul ^c   Bailey, David ^c   Cos, Paul ^d   Maes, Louis ^d   Adams, Emily ^e   Van Den Bogaart, Erika ^e   Chatelain, Eric ^f   Ioset, Jean Robert ^f   Van De Stolpe, Andrea ^a   Zorg, Stèphanie ^a   Veerman, Johan ^g   Seebeck, Thomas ^b   Sterk, Geert Jan ^g   De Esch, Iwan J P ^a   Leurs, Rob ^a   more..

^a AMSTERDAM INSTITUTE FOR MOLECULES   (Netherlands)

^b UNIVERSITY OF BERN   (Switzerland)

^c St John's Innovation Centre   (United Kingdom)

^d UNIVERSITY OF ANTWERP   (Belgium)

^e ROYAL TROPICAL INSTITUTE   (Netherlands)

^f DND i (Drugs for Neglected Diseases Initiative)   (Switzerland)

^g Mercachem BV   (Netherlands)

^h Swiss Transfusion SRC Inc   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ANTITRYPANOSOMAL AGENT; CATECHOL PYRAZOLINONE; CYCLIC AMP; TRYPANOSOMAL PHOSPHODIESTERASE B1 INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG SYNTHESIS; FLUORESCENCE RESONANCE ENERGY TRANSFER; IC 50; KINETOPLAST; NONHUMAN; PHENOTYPE; TRYPANOSOMA RHODESIENSE;

BINDING SITES; CATECHOLS; CYCLIC AMP; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 1; DRUG DESIGN; MOLECULAR DOCKING SIMULATION; PYRAZOLES; PYRAZOLONES; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAZOLES; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMA BRUCEI RHODESIENSE;

EID: 84867796428     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301059b     Document Type: Article

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