Abstract
Quinazolinones have pharmacological effects on vascular reactivity through different mechanisms. We synthesized 4-phenylquinazolin-2(1H)-one derivatives under microwave irradiation and tested them on the rat thoracic aorta. The prepared compounds 2a–2f were obtained in about 1 h with suitable yields (31–92%). All derivatives produced vasorelaxant effects with IC50 values ranging from 3.41 ± 0.65 µM to 39.72 ± 6.77 µM. Compounds 2c, 2e and 2f demonstrated the highest potency in endothelium-intact aorta rings (IC50 4.31 ± 0.90 µM, 4.94 ± 1.21 µM and 3.41 ± 0.65 µM respectively), and they achieved around 90% relaxation (30 μM). In aorta rings without an endothelium, the effect of compound 2f was abolished. Using the MTT assay to test for cell viability, only compound 2b induced cytotoxicity at the maximum concentration employed (30 µM). The results show that vasorelaxation by 4-phenylquinazolin-2(1H)-one derivatives might depend on the activation of a signalling pathway triggered by endothelium-derived factors.
Highlights
Heterocyclic drugs make up over 60% of major retail medicines for the pharmaceutical market [1,2].Considering the heterocyclic quinazolines and quinazolinone-containing compounds, they have already shown pharmacological relevance with broad therapeutic potential [3]
Drugs alpha 1-adrenergic (α1) receptor antagonists used in the treatment of hypertension [6,7]. Drugs such such as prazosin or terazosin vascular smooth muscle receptors,leading leadingtotovasodilation vasodilation and and aa as prazosin or terazosin act act on on vascular smooth muscle receptors, consequent reduction in peripheral vascular resistance; these medications are used for the treatment of consequent reduction in peripheral vascular resistance; these medications are used for the treatment benign prostatic hyperplasia (BPH)
Several methodologies for the 4-phenylquinazolin-2(1H)-one scaffold have been described in Several methodologies the 4-phenylquinazolin-2(1H)-one scaffold have beenreagents described in the the literature; theyfor require prolonged reaction times [16,17]
Summary
Heterocyclic drugs make up over 60% of major retail medicines for the pharmaceutical market [1,2]. Drugs alpha 1-adrenergic (α1) receptor antagonists used in the treatment of hypertension [6,7] Drugs such such as prazosin or terazosin vascular smooth muscle receptors,leading leadingtotovasodilation vasodilation and and aa as prazosin or terazosin act act on on vascular smooth muscle receptors, consequent reduction in peripheral vascular resistance; these medications are used for the treatment of consequent reduction in peripheral vascular resistance; these medications are used for the treatment benign prostatic hyperplasia (BPH). Several therapeutic activities ofand quinazolines and their derivatives haveinbeen literature, including antimicrobial [12], antitumor [13,14].
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