Current medicinal chemistry · 2025
Imine Derivatives of Hydrochlorothiazide Bear Potential Diuretic Activity in in vivo Experimental Model by Targeting Renal Outer Medullary Potassium Channel.
СтатьяНазвание и аннотация: Перевод в очереди
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Warda Hafiza Saliha, Sultana Kishwar, Ullah Irfan, Jan Afnan, Abdellattif Magda H, Kashtoh Hamdy, Ur Rehman Najeeb, Khan Ajmal, Al-Harrasi Ahmed
Аннотация
INTRODUCTION: This study involves several recently synthesized Schiff base derivatives of hydrochlorothiazide (3a-3e), characterized by advanced spectroscopic techniques including Fourier transform infrared (FTIR), 1H-, 13C-NMR (Nuclear magnetic resonance), and High-resolution electrospray ionization mass spectrometry (HR-ESI-MS).
METHODS: Hydrochlorothiazide (HCTZ, 2 mM) was mixed with 2 mM aldehydes in ethanol (20 mL) in the presence of glacial acetic acid, and the product was stirred with the help of a magnetic stirrer under the specified conditions. Keeping in mind the importance of imine derivatives against DPPH radical, the synthesized compounds were evaluated for antioxidant activity (in vitro) using DPPH assay and diuretic activity (in vivo) by Lipschitz method. All derivatives demonstrated notable antioxidant activity, exhibiting 52-86% inhibition.
RESULTS: The compounds 3a-3e also displayed remarkable diuretic effects in an in vivo model at a dose of 50 mg/kg. The computational studies of all the newly synthesized compounds were interpreted for the diuretic activity at the molecular level against human renal outer medullary potassium channel (ROMK1, PDB: ID) protein present on the nephron involved in diuresis indicating all compounds showed significant interactions at all receptors.
CONCLUSION: As the derivatives were more active than drugs in some regards; therefore, these derivatives will be beneficial and open new windows for research and additional pharmacological screening could be planned as part of the project's extension.
METHODS: Hydrochlorothiazide (HCTZ, 2 mM) was mixed with 2 mM aldehydes in ethanol (20 mL) in the presence of glacial acetic acid, and the product was stirred with the help of a magnetic stirrer under the specified conditions. Keeping in mind the importance of imine derivatives against DPPH radical, the synthesized compounds were evaluated for antioxidant activity (in vitro) using DPPH assay and diuretic activity (in vivo) by Lipschitz method. All derivatives demonstrated notable antioxidant activity, exhibiting 52-86% inhibition.
RESULTS: The compounds 3a-3e also displayed remarkable diuretic effects in an in vivo model at a dose of 50 mg/kg. The computational studies of all the newly synthesized compounds were interpreted for the diuretic activity at the molecular level against human renal outer medullary potassium channel (ROMK1, PDB: ID) protein present on the nephron involved in diuresis indicating all compounds showed significant interactions at all receptors.
CONCLUSION: As the derivatives were more active than drugs in some regards; therefore, these derivatives will be beneficial and open new windows for research and additional pharmacological screening could be planned as part of the project's extension.