Current status of antihistamine drugs repurposing for infectious diseases

Travi, Bruno L.

doi:10.1016/j.medidd.2022.100140

Cited by 9 publications

(2 citation statements)

References 112 publications

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“…The endeavor to discover approved drugs that exhibit in vitro efficacy against Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV-2) led to the identification of antiviral sigma-1 receptor ligands, which include antihistamines. [1][2][3] Chlorphenoxamine hydrochloride (CPX):2-[(4chlorophenyl)1phenylethoxy]-N, N-dimethyl ethanamine, as shown in supporting information Fig. S-1, is a compound that has gained attention for its remarkable anti-histaminic and anti-cholinergic properties.…”

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confidence: 99%

“…2 Supported by FDA approval for off-label uses, CPX has emerged as a promising tool in combating various deadly viral infections, including SARS-CoV, Middle East Respiratory Syndrome Coronavirus (MERS-CoV), and Ebola Virus (EBOV), primarily due to its exceptional capabilities as a G Protein-coupled receptor antagonist. 1,3 The ability to detect CPX at very low quantities in biological fluids is extremely valuable for identifying cases of overdose, especially when unintentional consumption by children occurs.…”

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Novel Green Screen-Printed Potentiometric Sensor for Monitoring Antihistamine Drug Chlorphenoxamine HCl in Various Matrices

Ashraf,

El-Zeany,

Sedik

et al. 2024

J. Electrochem. Soc.

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The pharmaceutical sector is seeking cost-effective analyzers that deliver precise, real-time data. This study aims to establish a correlation between the pharmaceutical industry and advancements in solid-contact ion-selective electrodes for quantifying chlorphenoxamine hydrochloride (CPX) concentration in various matrices. A comparative analysis of the performance between solid contact and liquid contact sensors showed that solid contact sensors outperformed their liquid contact counterparts in terms of durability, handling, and ease of integration. A sensor was developed using MWCNT and calix[8]arene as ionophore, resulting in a Nernstian potentiometric response for CPX across a linear range of 5.0×10−5 to 1.0×10−8 M. The slope of the response was 57.89 ± 0.77 mV/decade, and the standard potential was determined to be 371.9 ± 0.8 mV. The developed sensor exhibits notable intrinsic advantages, such as a rapid response time of 12 ± 2 seconds and an extended lifespan of 3 months. The sensor exhibiting optimal performance has been effectively employed for the analysis of CPX in different matrices, including pharmaceutical formulations, urine, and plasma. The developed method underwent validation in compliance with ICH requirements. Finally, the method’s greenness and whiteness were evaluated using five different tools and successfully compared to those obtained from the established reported method.

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confidence: 99%

Novel Green Screen-Printed Potentiometric Sensor for Monitoring Antihistamine Drug Chlorphenoxamine HCl in Various Matrices

Ashraf,

El-Zeany,

Sedik

et al. 2024

J. Electrochem. Soc.

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Designing and Synthesis of Novel Fexofenadine‐Derived Hydrazone‐Schiff Bases as Potential Urease Inhibitors: In‐Vitro, Molecular Docking and DFT Investigations

Ayaz,

Alam,

Zainab

et al. 2024

Chemistry & Biodiversity

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Thirteen novel hydrazone‐Schiff bases (3‐15) of fexofenadine were succesfully synthesized, structurally deduced and finally assessed their capability to inhibit urease enzyme (in vitro). In the series, six compounds 12 (IC50 = 10.19 ± 0.16 µM), 11 (IC50 = 15.05 ± 1.11 µM), 10 (IC50 = 17.01 ± 1.23 µM), 9 (IC50 = 17.22 ± 0.81 µM), 13 (IC50 = 19.31 ± 0.18 µM), and 14 (IC50 = 19.62 ± 0.21 µM) displayed strong inhibitory action better than the standard thiourea (IC50 = 21.14 ± 0.24 µM), while the remaining compounds displayed significant to less inhibition. LUMO and HOMO showed the transferring of charges from molecules to biological transfer and MEP map showed the chemically reactive zone appropriate for drug action are calculated using DFT. AIM charges, non‐bonding orbitals, and ELF are also computed. The urease protein binding analysis benefited from the docking studies.

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