Mini-Reviews in Medicinal Chemistry, Vol 18, No 10 (2018)

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A review of the pharmacological properties of 3,4-dihydro-2(1H)-quinolinones

Ms. Letitia Meiring, Prof. Jacobus P Petzer, Prof. Anél Petzer


The 3,4-dihydro-2(1H)-quinolinone moiety is present in a number of pharmacologically active compounds. These include registered 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 en 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.


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