Long-chain fatty dihydropyridines: Docking calcium channel studies and antihypertensive activity

Santa-Helena, Eduarda; Cabrera, Diego da Costa; D’Oca, Marcelo Gonçalves Montes; Scaini, João L.; Oliveira, Matheus William Bandeira de; Werhli, Adriano Velasque; Machado, Karina; Gonçalves, Carla Amorim Neves; Nery, Luiz Eduardo Maia

doi:10.1016/j.lfs.2020.118210

Cited by 4 publications

(3 citation statements)

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“…These results [18] demonstrated that several synthesized fatty DHPs improved antioxidant potential when compared to standard pharmaceutical nifedipine, and tests in cardioblast culture demonstrate that these compounds have cardioprotector effects after ischemia and reperfusion [12,17]. In a current study by Santa-Helena et al [19], it has been shown that these fatty DHPs continue to interact with calcium channels, and in addition, these molecules are non-toxic during and after 56 days of treatment. Other dihydropyridine derivatives have been proven to protect the heart from ischemic injury and atherosclerosis [20], due to the capacity to inhibit L-type calcium channel and differentiated cardiac depressive action [21].…”

Section: Introductionmentioning

confidence: 74%

“…The groups were subdivided into control and group I/R that received a solution of the vehicle (DMSO 1%, 1 mL/400 g of weight) for 8 weeks; Group high blood pressure (HBP + I/R) received pretreatment with L-NAME (10 mg/kg/day); Group nifedipine and L-NAME (HBP + nifedipine + I/R) received at the same time pretreatment with L-NAME (10 mg/kg/day) and nifedipine (0.42 mg/kg/day). The remaining groups received pretreatment with a combination of L-NAME (10 mg/kg/day) and one of the new compounds: 2c (HBP + 2c + I/R), 8c (HBP + 8c + I/R), and 9a (HBP + 9a + I/R) all at a concentration of 0.42 mg/kg/day (same concentration used by Santa-Helena et al [19]. The experiments with isolated hearts were performed 24h after the last administration of drugs using a retrograde perfusion system for all groups with exception of the control group, as described in 2.6.…”

Section: Pharmacological Induction Of Hypertension and Treatmentsmentioning

confidence: 99%

“…Figure 1 Schematic images of fatty dihydropyridines tested in this study [12,18,19]. Figure 2 Schematic illustration of the experimental protocol for ischemia and reperfusion in isolated hearts.…”

Section: Declarations Figuresmentioning

confidence: 99%

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Fatty Dihydropyridines With Anti-Hypertensive and Cardioprotective Potential During Ischemia and Reperfusion

Santa-Helena

Ribeiro

Gioda

et al. 2021

Preprint

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In this study, three fatty dihydropyridines, were tested for their anti-hypertensive and cardioprotective properties. Dihydropyridines 2c, 8c, and 9a contain the oleic chain and the nitro unit, the oleic chain and the chlorine unit, and the palmitic chain and the chlorine unit, respectively. For the experiments, animals were treated with N(ω)-nitro-L-arginine methyl ester to induce hypertension and after treated with the new dihydropyridine compounds and the standard drug nifedipine. Then, the heart was removed and subjected to global ischemia and reperfusion. Analyses of cardiac parameters were performed to monitor cardiac functionality; lactate dehydrogenase values were quantified in perfusates. After ischemia and reperfusion were performed, analyses to check the oxidative status and lipid damage. The results of the present study suggest that the new fatty DHPs have anti-hypertensive effects offering protection against ischemia to the heart of rats, accomplished by increasing antioxidants that defend and prevent the decline in cardiac function.

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Section: Introductionmentioning

confidence: 74%

Section: Pharmacological Induction Of Hypertension and Treatmentsmentioning

confidence: 99%

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Fatty Dihydropyridines With Anti-Hypertensive and Cardioprotective Potential During Ischemia and Reperfusion

Santa-Helena

Ribeiro

Gioda

et al. 2021

Preprint

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Fluorinated dihydropyridines as candidates to block L-type voltage-dependent calcium channels

Spadeto

Freitas

Cormanich

2021

Journal of Biomolecular Structure and Dynamics

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An Overview of Recent Advances in Hantzsch’s Multicomponent Synthesis of 1,4- Dihydropyridines: A Class of Prominent Calcium Channel Blockers

Kumar

Saini

Rani

et al. 2023

COC

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Among all the heterocyclic scaffolds, 1,4-dihydropyridine (1,4-DHPs) is an important class of nitrogen-containing heterocyclic compounds possessing prominent therapeutic effects, which play an essential role in pharmaceutical chemistry. Multicomponent reactions (MCRs) have proven to be an invaluable tool for swiftly synthesizing large and structurally diverse molecules from simple starting materials. The chemists have discovered a large number of new MCRs for the synthesis of 1,4-dihydropyridine. The synthesis of 1,4-Dihydropyridine via multicomponent reaction is an efficient procedure in terms of delivering adequate structural diversity, which is essential for the process of discovering new 1,4-DHPs compounds and their therapeutics.1,4-dihydropyridines are well-known L-type calcium channel blockers. This review aims to study and summarize the recent developments in the multicomponent synthesis of 1,4-dihydropyridines and their fused analogs that act as potent antihypertensive drugs. The findings of this study will prove to be an invaluable resource for researchers in the areas of heterocyclic chemistry, medicinal chemistry, and drug design.

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Long-chain fatty dihydropyridines: Docking calcium channel studies and antihypertensive activity

Cited by 4 publications

References 50 publications

Fatty Dihydropyridines With Anti-Hypertensive and Cardioprotective Potential During Ischemia and Reperfusion

Fatty Dihydropyridines With Anti-Hypertensive and Cardioprotective Potential During Ischemia and Reperfusion

Fluorinated dihydropyridines as candidates to block L-type voltage-dependent calcium channels

An Overview of Recent Advances in Hantzsch’s Multicomponent Synthesis of 1,4- Dihydropyridines: A Class of Prominent Calcium Channel Blockers

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