Cyclopentanespiro-3H-dihydro-pyrimidinones as Angiotensin II AT1 receptor antagonists

Bernhart, C.; Hundricourt, F.B.; Assens, J.‐L. A.; Gougat, J.; Lacour, Colette; Roccon, Alain; Cazaubon, Catherine; Brelière, Jean-Claude; Fur, G. Le; Nisato, Dino

doi:10.1016/s0960-894x(01)81139-2

Cited by 6 publications

(3 citation statements)

References 2 publications

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“…Additionally, it was reported that the reaction involving the synthesis of 4-amino-1, 2, 4-triazole can took place by a simple conversion of 1, 3, 4-oxadiazole under the action of hydrazine hydrate [24,25]. Likewise, the corresponding dicarbonyl compounds including acetylacetone and ethyl acetoacetate were subjected to condensation with acid hydrazide (6) 21), respectively (Figure 4). The structure of these compounds was established based on spectral and elemental analysis reported in the related literature [26][27][28].…”

Section: Compound Name Ketones Aldehydesmentioning

confidence: 99%

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2018

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Section: Compound Name Ketones Aldehydesmentioning

confidence: 99%

“…The pyrimidinones compounds have gained interest in recent years due to their wide-ranging biological activity. These compounds displayed therapeutic applications, as anticancer [4,5], antihypertensive [6], hypoglycaemic [7], antiviral [8], anticonvulsive [9], anti-inflammatory and analgesic [10] drugs.…”

Section: Introductionmentioning

confidence: 99%

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2018

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“…Pyrimidinone derivatives are well-known for their pharmacological properties [ 1 , 2 ]. These compounds, structurally related to nucleic acids, have been reported to be anticancer [ 3 , 4 , 5 , 6 , 7 ], interferon inducer [ 8 ], antiviral [ 9 , 10 ], anti-hypertensive [ 11 , 12 ], hypoglycaemic [ 13 , 14 ], anticonvulsive [ 15 ], anti-histaminic [ 16 ], analgesic and antiinflammatory drugs [ 17 , 18 , 19 , 20 , 21 , 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

Comparative Computational Studies of 3,4-Dihydro-2,6-diaryl-4-oxo-pyrimidine-5-carbonitrile Derivatives as Potential Antinociceptive Agents

et al. 2012

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In this study, the antinociceptive properties of 3,4-dihydro-2,6-diaryl-4-oxo-pyrimidine-5-carbonitrile derivatives 5a–i at doses of 25 and 50 mg/kg were evaluated in mice, using the abdominal constriction test. Molecular modeling studies were also performed using density functional theory calculations. These data provided information about the electrostatic and ionization potentials and were used to compare the antinociceptive activity of the title compounds. The most active compounds were 3,4-dihydro-2-(4-chlorophenyl)-6-(4-methoxyphenyl)-4-oxo-pyrimidine-5-carbonitrile (5b) and 3,4-dihydro-2,6-diphenyl-4-oxo-pyrimidine-5-carbonitrile (5i), which inhibited the number of abdominal constrictions, at 50 mg/kg dose, in 88.6% and 88% of the sample, respectively. A preliminary SAR study demonstrated that halogen replacement in the phenyl rings of the compounds under study reduces the antinociceptive activity. DFT calculations showed that there is a high correlation between the ionization potentials and the analgesic properties of the compounds. It was found that compounds with a positive ionization potential (compounds 5b and 5i) were found to be the best analgesic drugs in this series.

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New Pyrimidinone and Fused Pyrimidinone Derivatives as Potential Anticancer Chemotherapeutics

Rashad

Shamroukh

Yousif

et al. 2012

Archiv der Pharmazie

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A series of novel substituted pyrimidinones and fused pyrimidinones (compounds 3-18) were synthesized starting with oxiranylmethanone 2. The in vitro cytotoxicity against a human breast adenocarcinoma (MCF-7) cell line was investigated and most of the tested compounds showed potent cytotoxic activity against the MCF-7 cell line comparable to the activity of the commonly used anticancer drug cisplatin. Treatment of MCF-7 cells with increasing doses (2, 5, 10, and 20 µg/mL) of the tested compounds revealed that the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered compared with control MCF-7 cells. In general, derivatives 11 and 16 revealed the highest anticancer activity among the tested compounds.

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Cyclopentanespiro-3H-dihydro-pyrimidinones as Angiotensin II AT1 receptor antagonists

Cited by 6 publications

References 2 publications

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Comparative Computational Studies of 3,4-Dihydro-2,6-diaryl-4-oxo-pyrimidine-5-carbonitrile Derivatives as Potential Antinociceptive Agents

New Pyrimidinone and Fused Pyrimidinone Derivatives as Potential Anticancer Chemotherapeutics

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