The 3,4-dihydro-2(1H)-quinolinone moiety is present in a number of pharmacologically active
compounds. These include FDA approved drugs such as cilostazol, carteolol and aripiprazole as
well as numerous experimental compounds. Compounds containing the 3,4-dihydro-2(1H)-quinolinone
moiety also exhibit a variety of activities in both the peripheral and central tissues, which includes
phosphodiesterase inhibition, blocking of β-adrenergic receptors, antagonism of vasopressin receptors
and interaction with serotonin and dopamine receptors. Based on its versatility in drug design and action,
this paper reviews the pharmacological actions of compounds containing the 3,4-dihydro-2(1H)-
quinolinone scaffold with emphasis being placed on the most important and significant members of
each activity class.
Keywords: Aripiprazole, carteolol, cilostazol, 3, 4-dihydro-2(1H)-quinolinone, pharmacology, drug design.
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