@article{46243be7709f4e4c8c2e9a615f593808,
title = "Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase b1",
abstract = "Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), also known as African sleeping sickness. We used homology modeling and docking studies to guide fragment growing into the parasite-specific P-pocket in the enzyme binding site. The resulting catechol pyrazolinones act as potent TbrPDEB1 inhibitors with IC",
author = "K.M. Orrling and C.J.W. Jansen and X.L. Vu and V. Balmer and P. Bregy and A. Shanmugham and P. England and D. Bailey and P. Cos and L. Maes and E. Adams and {van den Bogaart}, E. and E. Chatelain and J.R. Ioset and {van de Stolpe}, A. and S. Zorg and J. Veerman and T. Seebeck and G.J. Sterk and {de Esch}, I.J.P. and R. Leurs",
year = "2012",
doi = "10.1021/jm301059b",
language = "English",
volume = "55",
pages = "8745--8756",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
}