Amata Emanuele, Bland Nicholas D, Campbell Robert K, Pollastri Michael P
Northeastern University Department of Chemistry and Chemical Biology, 417 Egan Research Center, 360 Huntington Avenue, Boston, MA 02115, USA.
Marine Biological Laboratory, Josephine Bay Paul Center for Comparative Molecular Biology and Evolution, 7 MBL Street, Woods Hole, MA 02543, USA.
Tetrahedron Lett. 2015 May 20;56(21):2832-2835. doi: 10.1016/j.tetlet.2015.04.061.
Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen , which affects thousands every year and which is in need of new therapeutics. Herein we report the synthesis and assessment of a series of pyrrolidine and pyrazolone derivatives of human phosphodiesterase 4 (hPDE4) inhibitors for the assessment of their activity against the trypanosomal phosphodiesterase TbrPDEB1. The synthesized compounds showed weak potency against TbrPDEB1.
人类非洲锥虫病（HAT）是一种由原生动物病原体引起的寄生虫病，每年影响数千人，并且需要新的治疗方法。在此，我们报告了一系列人磷酸二酯酶4（hPDE4）抑制剂的吡咯烷和吡唑啉酮衍生物的合成与评估，以评估它们对锥虫磷酸二酯酶TbrPDEB1的活性。合成的化合物对TbrPDEB1显示出较弱的效力。
