Experimental and computational pharmacological approaches decoding the anti-diabetic molecular mechanism of indole based triazole bearing sulfonothioate derivatives

In search for a potent anti-Diabetes therapeutic agent, we have synthesized a series of indole based triazole derived sulfonothioate derivatives (1–15). These compounds were structurally elucidated via different techniques like 1HNMR, 13CNMR, and HREI-MS. Biological potential of all the derivatives against diabetes mellitus was contrasted with the reference drug Acarbose. In this regard, analog 7 (IC50 = 3.20 ± 0.10 and 4.20 ± 0.50 µM), 9 (IC50 = 5.10 ± 0.10 and 5.70 ± 0.30 µM) and 15 (IC50 = 3.20 ± 0.70 and 3.40 ± 0.50 µM) emerged as the leading inhibitor with captivating potential in comparison to standard drug acarbose (IC50 = 10.40 ± 0.50 and 11.50 ± 0.20 µM). Structure activity relationship determined the influence of substitution (−F, −Cl, –OH, NO2 etc.) on drug profile of the synthesized analogs. Drug profile of these compounds was also analyzed through molecular docking investigations, assessing the bonding interactions between ligands and enzymes. Furthermore, ADME analysis was performed on the promising compounds, revealing traits akin to those of pharmaceuticals.

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Publication Details

Journal
Results in Chemistry
Published
2024-08-01
DOI
https://doi.org/10.1016/j.rechem.2024.101707
Citations
8
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
2.00
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Experimental and computational pharmacological approaches decoding the anti-diabetic molecular mechanism of indole based triazole bearing sulfonothioate derivatives

Alanood S. Algarni, Rafaqat Hussain, Hayat Ullah, Yousaf Khan et al.
8 citations
Results in Chemistry
Synthesis and biological activity
2.00
article

Experimental and computational pharmacological approaches decoding the anti-diabetic molecular mechanism of indole based triazole bearing sulfonothioate derivatives

Alanood S. Algarni, Rafaqat Hussain, Hayat Ullah, Yousaf Khan, Tayyaba Zahoor, Rashid Iqbal, Shoaib Khan, Muhammad Saleem Khan, Tayyiaba Iqbal, Lena W.M. Abdelmageed, Zanib Fiaz, M.Y. Siraj
article en
8 citations

Abstract

In search for a potent anti-Diabetes therapeutic agent, we have synthesized a series of indole based triazole derived sulfonothioate derivatives (1–15). These compounds were structurally elucidated via different techniques like 1HNMR, 13CNMR, and HREI-MS. Biological potential of all the derivatives against diabetes mellitus was contrasted with the reference drug Acarbose. In this regard, analog 7 (IC50 = 3.20 ± 0.10 and 4.20 ± 0.50 µM), 9 (IC50 = 5.10 ± 0.10 and 5.70 ± 0.30 µM) and 15 (IC50 = 3.20 ± 0.70 and 3.40 ± 0.50 µM) emerged as the leading inhibitor with captivating potential in comparison to standard drug acarbose (IC50 = 10.40 ± 0.50 and 11.50 ± 0.20 µM). Structure activity relationship determined the influence of substitution (−F, −Cl, –OH, NO2 etc.) on drug profile of the synthesized analogs. Drug profile of these compounds was also analyzed through molecular docking investigations, assessing the bonding interactions between ligands and enzymes. Furthermore, ADME analysis was performed on the promising compounds, revealing traits akin to those of pharmaceuticals.

Results in ChemistryVol. 10
COMSATS University Islamabad (PK), Hunan University (CN), Islamia University of Bahawalpur (PK), Umm al-Qura University (SA), King Saud University (SA), University of Okara (PK), Western Caspian University (AZ), Abbottabad University of Science and Technology (PK)
Zero hunger
Openalex Percentile: Top 14%
Synthesis and biological activity
2.00
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