Ontology highlight
ABSTRACT:
SUBMITTER: Li J
PROVIDER: S-EPMC3625062 | biostudies-literature | 2013 Feb
REPOSITORIES: biostudies-literature
Li Junfeng J Jin Hongjun H Zhou Haiying H Rothfuss Justin J Tu Zhude Z
MedChemComm 20130201 2
Twenty eight new analogues were synthesized by optimizing the structure of <b>MP-10</b> and their <i>in vitro</i> binding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues, <b>10a</b>, <b>10b</b>, <b>10d</b>, <b>11a</b>, <b>11b</b> and <b>11d</b> are very potent towards PDE10A and have IC<sub>50</sub> 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 fo ...[more]