title: Synthesis andin vitrobiological evaluation of pyrazole group-containing analogues for PDE10A.
abstract: Twenty eight new analogues were synthesized by optimizing the structure ofMP-10and theirin vitrobinding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues,10a,10b,10d,11a,11band11dare very potent towards PDE10A and have IC50values of 0.40 ± 0.02, 0.28 ± 0.06, 1.82 ± 0.25, 0.24 ± 0.05, 0.36 ± 0.03 and 1.78 ± 0.03 nM respectively; these six compounds displayed high selectivity for PDE10AversusPDE3A/3B/4A/4B. The promising compounds will be further validatedin vivoto identify PDE10A imaging tracers.
authors.affiliation: Department of Radiology, Washington University School of Medicine, St. Louis, MO, 63110, USA; ; Tel: +1-314-362-8487.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Li
authors.forename: Hongjun
authors.initials: H
authors.lastname: Jin
authors.forename: Haiying
authors.initials: H
authors.lastname: Zhou
authors.forename: Justin
authors.initials: J
authors.lastname: Rothfuss
authors.forename: Zhude
authors.initials: Z
authors.lastname: Tu