Antihypertensive potential of selected pyrimidine derivatives: Explanation of underlying mechanistic pathways

Irshad, Nadeem; Khan, Arif‐ullah; Alamgeer, -; Khan, Salah-Ud-Din; Iqbal, Muhammad Shahid

doi:10.1016/j.biopha.2021.111567

Cited by 28 publications

(20 citation statements)

References 38 publications

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“…The LPO level was analyzed by its resultant end product called malondialdehyde (MDA). Microplate reader was used to measure the absorbance at wavelength of 532 nm where quantitative measurement of LPO was expressed in TBARS nmoles/min/mg of protein [25].…”

Section: Anti-oxidant Profilementioning

confidence: 99%

“…Images of slides were taken using a light microscope (Olympus, Japan) and analyzed through Image J, a computer-based program, while focusing thoroughly on gastric cell size and shape, inflamed infiltrated cells, and vacuolation. The TIF images were arranged to the same threshold intensity for all groups and examined in the GraphPad Prism.8 [25].…”

Section: Hematoxylin and Eosin (Hande) Stainingmentioning

confidence: 99%

“…Image J software was used for the quantitative determination of hyperactivated p-NFκB, COX-2 and TNF-α by optimizing the background of images according to the threshold intensity and analyzing p-NFκB, COX-2 and TNF-α positive cells at the same threshold intensity for all groups. The intensity is expressed as the relative integrated density of the samples relative to the saline [25].…”

Section: Immunohistochemistry (Ihc)mentioning

confidence: 99%

“…To visualize the immuno-reactive bands, an enhanced western blotting substrate kit was used. Using Image J software, densitometry evaluated the quantification of protein expression [25].…”

Section: Western Blotmentioning

confidence: 99%

“…The firststrand of cDNA was generated from 1 to 2 μg of total RNA by a reverse transcriptase enzyme mix on a PCR thermocycler. The mRNA expression normalized to the expression of β-Actin as a house-keeping gene by 2 -∆∆ CT method with slight modification [25]. Primer sequences for β-Actin and H + /K + -ATPase were CCC GCG AGT ACA ACC TTC T (forward) and CGT CAT CCA TGG CGA ACT (reverse) and TAT GAA TTG TAC TCA GTG GA (forward) and TGG TCT GGT ACT TCT GCT (reverse), respectively.…”

Section: Real Time Polymerase Chain Reaction (Rt-pcr)mentioning

confidence: 99%

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Pharmacological evaluation of newly synthesized organotin IV complex for antiulcer potential

Azmatullah

Khan

Qazi

et al. 2022

BMC Pharmacol Toxicol

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The present study aims to investigate the newly synthesized organotin (IV) complex (2E, 2′E) dibutylstannanediyl bis (4-(4-nitrophenyl) amino)-4-oxobut-2-enoate (DTN) for its anti-ulcer potential. Characterization performed by carbon nuclear magnetic resonance spectroscopy proved that all values are in the expected ranges of the new compound. Gastroprotective activity of DTN was evaluated through in-silico, anti-H. pylori, in-vitro, in-vivo, and ex-vivo proteomic analysis. In-silico analysis shows that DTN possess stable binding with protein targets involved in gastric ulcer pathophysiology. DTN exhibited an inhibitory effect against 2,2-diphenyl-1-picrylhydrazyl, H. pylori and hydrogen potassium ATPase (H+/K+-ATPase). The antiulcer activity was performed using an ethanol-induced gastric ulcer model in rats. Anti-oxidant profile of DTN showed a significant increase in glutathione-S-transferase, glutathione and catalase levels whereas lipid peroxidation levels were reduced. Histopathological findings confirmed that DTN protected the gastric mucosa of rats. Inflammatory markers tumor necrosis factor-alpha, nuclear factor kappa B, cyclooxygenase-2, interleukin 6 and interleukin-1β were reduced and prostaglandin-E2 restored expression of these cytokines in DTN pretreated animals when analyzed by using immunohistochemistry, enzyme-linked immunosorbent assay and western blot techniques. In real-time polymerase chain reaction technique, the expression of H+/K+-ATPase was downregulated in DTN pretreated group. DTN did not cause any mortality up to 400 mg/Kg. This study indicates that the newly synthesized compound DTN, possess stable binding against selected targets. DTN exhibits a gastro-protective effect, mediated via anti-H. pylori, H+/K+-ATPase inhibition, anti-oxidant and anti-inflammatory pathways, exploring its therapeutic potential in gastric ulcer management.

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Section: Anti-oxidant Profilementioning

confidence: 99%

Section: Hematoxylin and Eosin (Hande) Stainingmentioning

confidence: 99%

Section: Immunohistochemistry (Ihc)mentioning

confidence: 99%

“…To visualize the immuno-reactive bands, an enhanced western blotting substrate kit was used. Using Image J software, densitometry evaluated the quantification of protein expression [25].…”

Section: Western Blotmentioning

confidence: 99%

Section: Real Time Polymerase Chain Reaction (Rt-pcr)mentioning

confidence: 99%

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Pharmacological evaluation of newly synthesized organotin IV complex for antiulcer potential

Azmatullah

Khan

Qazi

et al. 2022

BMC Pharmacol Toxicol

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Antioxidant and Antimicrobial Activities of 4H‐Chromene Based Indole‐Pyrimidine Hybrids: Synthesis and Molecular Docking Studies

Vanga,

Bhukya,

Thumma

et al. 2024

Chemistry & Biodiversity

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A series of 4H‐Chromene Based Indole – Pyrimidine Hybrids synthesized using simple and efficient multicomponent reaction. The title molecules were evaluated for their invitro antioxidant and antimicrobial activities. Compounds 8g containing bromo substituted naphthalene displayed potent antioxidant activity with IC50 value of 1.09±0.34 µM and 1.10±0.36 µM. Compound 10a, a 4‐methylphenyl derivative presented potent activity with antioxidant activity with IC50 value of 1.29±0.35 µM and 1.43±0.38 µM. Subsequently, compounds 8a, 8b, 8d and 10g had shown prominent percentage of inhibition and derived effective IC50 values in comparison to reference drug Ascorbic Acid. The invitro antimicrobial activity carried out against two gram positive and two gram‐negative bacteria, and two fungal strains using Ampicillin and Itraconazole as refence drugs. Compound 10f exhibited exceptional efficacy against all types of bacterial and fungal strains compared to Ampicillin and Itraconazole, compounds 8e and 8g showed activity against bacterial strains whereas compound 10g exhibited the most effective zone of inhibition against fungal strains. The molecular docking study against crystal structure of NADPH oxidase obtained supporting docking scores and showed notable binding interactions such as H‐bond and hydrophobic.

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Chalcones: Versatile intermediates in heterocyclic synthesis

Nayak

Gaonkar

Sabu

2023

Journal of Heterocyclic Chem

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Chalcones are a fascinating and well‐studied group of organic molecules. Synthesis of chalcones has been one of the essential areas of organic synthesis over the last few decades because of their immense therapeutic and excellent photophysical properties. Furthermore, these chalcone derivatives can be utilized to make a variety of heterocyclic compounds, especially five‐ and six‐membered heterocycles. Heterocyclic compounds have a long history in chemistry, primarily in pharmaceuticals. However, synthesizing some specific heterocyclic molecules remains challenging and requires multistep processes with few possible intermediates. Chalcones can be considered as one of the most useful, readily available intermediates in heterocyclic synthesis. Herein, the synthesis of various potential heterocyclic compounds using chalcones as an intermediate is elaborated. This review shows the untapped potential of chalcones in organic synthesis. Also, it will assist the chemist in designing new heterocycles by adopting these strategies.

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Antihypertensive potential of selected pyrimidine derivatives: Explanation of underlying mechanistic pathways

Cited by 28 publications

References 38 publications

Pharmacological evaluation of newly synthesized organotin IV complex for antiulcer potential

Pharmacological evaluation of newly synthesized organotin IV complex for antiulcer potential

Antioxidant and Antimicrobial Activities of 4H‐Chromene Based Indole‐Pyrimidine Hybrids: Synthesis and Molecular Docking Studies

Chalcones: Versatile intermediates in heterocyclic synthesis

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