Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth

G Andriani, E Amata, J Beatty, Z Clements…

Index: Andriani, Grasiella; Amata, Emanuele; Beatty, Joel; Clements, Zeke; Coffey, Brian J.; Courtemanche, Gilles; Devine, William; Erath, Jessey; Juda, Cristin E.; Wawrzak, Zdzislaw; Wood, Jodianne T.; Lepesheva, Galina I.; Rodriguez, Ana; Pollastri, Michael P. Journal of Medicinal Chemistry, 2013 , vol. 56, # 6 p. 2556 - 2567

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Citation Number: 41

Abstract

Chagas disease is caused by the intracellular protozoan parasite Trypanosomal cruzi, and current drugs are lacking in terms of desired safety and efficacy profiles. Following on a recently reported high-throughput screening campaign, we have explored initial structure– activity relationships around a class of imidazole-based compounds. This profiling has uncovered compounds 4c (NEU321) and 4j (NEU704), which are potent against in vitro ...