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Microwave Assisted Synthesis of 4-Phenylquinazolin-2(1H)-one Derivatives that Inhibit Vasopressor Tonus in Rat Thoracic Aorta

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Programa de Pós-Graduação em Ciências Aplicadas a Produtos para a Saúde, Faculdade de Farmácia, Universidade Federal Fluminense, Niterói 24241-000, RJ, Brazil
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Núcleo de Ciência Biomédicas Aplicadas, Instituto Federal do Rio de Janeiro, Rio de Janeiro 20270-021, RJ, Brazil
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Núcleo de Ciências Químicas, Instituto Federal do Rio de Janeiro, Rio de Janeiro 20270-021, RJ, Brazil
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(6), 1467; https://doi.org/10.3390/molecules25061467
Received: 12 February 2020 / Revised: 9 March 2020 / Accepted: 14 March 2020 / Published: 24 March 2020
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: microwave irradiation; 4-phenylquinazolin-2(1H)-one; vasorelaxation; endothelium; rat thoracic aorta microwave irradiation; 4-phenylquinazolin-2(1H)-one; vasorelaxation; endothelium; rat thoracic aorta
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MDPI and ACS Style

Teixeira, R.; Menengat, T.; Andrade, G.; Cotrim, B.; Ponte, C.; Santos, W.C.; Resende, G. Microwave Assisted Synthesis of 4-Phenylquinazolin-2(1H)-one Derivatives that Inhibit Vasopressor Tonus in Rat Thoracic Aorta. Molecules 2020, 25, 1467.

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