Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A

Junfeng Li, Hongjun Jin, Haiying Zhou, Justin Rothfuss, Zhude Tu

Research output: Contribution to journalArticle

13 Scopus citations

Abstract

Twenty eight new analogues were synthesized by optimizing the structure of MP-10 and their in vitro binding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues, 10a, 10b, 10d, 11a, 11b and 11d are very potent towards PDE10A and have IC50 values 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 PDE10A versus PDE3A/3B/4A/4B. The promising compounds will be further validated in vivo to identify PDE10A imaging tracers.

Original languageEnglish
Pages (from-to)443-449
Number of pages7
JournalMedChemComm
Volume4
Issue number2
DOIs
StatePublished - Feb 2013

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