TY - JOUR
T1 - Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A
AU - Li, Junfeng
AU - Jin, Hongjun
AU - Zhou, Haiying
AU - Rothfuss, Justin
AU - Tu, Zhude
N1 - Copyright:
Copyright 2015 Elsevier B.V., All rights reserved.
PY - 2013/2
Y1 - 2013/2
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84876729797&partnerID=8YFLogxK
U2 - 10.1039/c2md20239e
DO - 10.1039/c2md20239e
M3 - Article
AN - SCOPUS:84876729797
SN - 2040-2503
VL - 4
SP - 443
EP - 449
JO - MedChemComm
JF - MedChemComm
IS - 2
ER -