Theoretical insights into the reactivity, topological properties, and OSR1 kinase interaction of anti-hypertensive drugs: a DFT and docking-based study

A comprehensive theoretical investigation was carried out on two antihypertensive drugs, Hydrochlorothiazide (HCTZ) and Hydroflumethiazide (HFTZ), using Density Functional Theory (DFT) with the B3LYP-D3(BJ)/6-311++ G(d,p) hybrid functional including dispersion corrections.Hirshfeld surface analysis and fingerprint plots quantified intra- and intermolecular interactions, while the electron localization function (ELF) revealed atomic shell structures and localized lone pairs, especially around electronegative centers. Molecular docking studies highlighted significant binding interactions of both drugs with the OSR1 kinase protein, with HFTZ exhibiting superior inhibitory potential. Molecular dynamics simulations further confirmed the structural stability and interaction profiles of both drugs within the active site. HCTZ demonstrated a consistent interaction with GLY520, while HFTZ exhibited adaptive binding to the flexible loop regions, especially interacting with LEU473 through its sulfonamide group. These findings provide deep insights into the structural, electronic, and binding characteristics of these antihypertensive agents, supporting their pharmacological relevance and guiding future drug design strategies. This comparative framework highlights how subtle structural variations, such as fluorine substitution in HFTZ, influence electronic delocalization and binding behaviour.

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Publication Details

Journal
Discover Chemistry.
Published
2026-01-03
DOI
https://doi.org/10.1007/s44371-025-00389-4
Citations
1
Primary Topic
Crystallography and molecular interactions
Type
article
Field-Weighted Citation Impact
26.05
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article

Theoretical insights into the reactivity, topological properties, and OSR1 kinase interaction of anti-hypertensive drugs: a DFT and docking-based study

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Discover Chemistry.
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article

Theoretical insights into the reactivity, topological properties, and OSR1 kinase interaction of anti-hypertensive drugs: a DFT and docking-based study

Niranjana Devi Rajendran, Arulraj Ramalingam, Srinivas Ganjipete, Justin Prabakaran, Ronaldo Anuf, Parasuraman Pavadai
article en
1 citations

Abstract

A comprehensive theoretical investigation was carried out on two antihypertensive drugs, Hydrochlorothiazide (HCTZ) and Hydroflumethiazide (HFTZ), using Density Functional Theory (DFT) with the B3LYP-D3(BJ)/6-311++ G(d,p) hybrid functional including dispersion corrections.Hirshfeld surface analysis and fingerprint plots quantified intra- and intermolecular interactions, while the electron localization function (ELF) revealed atomic shell structures and localized lone pairs, especially around electronegative centers. Molecular docking studies highlighted significant binding interactions of both drugs with the OSR1 kinase protein, with HFTZ exhibiting superior inhibitory potential. Molecular dynamics simulations further confirmed the structural stability and interaction profiles of both drugs within the active site. HCTZ demonstrated a consistent interaction with GLY520, while HFTZ exhibited adaptive binding to the flexible loop regions, especially interacting with LEU473 through its sulfonamide group. These findings provide deep insights into the structural, electronic, and binding characteristics of these antihypertensive agents, supporting their pharmacological relevance and guiding future drug design strategies. This comparative framework highlights how subtle structural variations, such as fluorine substitution in HFTZ, influence electronic delocalization and binding behaviour.

Discover Chemistry.Vol. 3(1)
Madurai Kamaraj University (IN), M S Ramaiah University of Applied Sciences (IN), Noorul Islam University (IN)
Good health and well-being
Openalex Percentile: Top 3%
Crystallography and molecular interactions
26.05
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