2,3-Dihydrosorbicillin and chrysopanol stimulate insulin secretion in INS-1 cells

Lee, Dahae; Kim, Jae‐Kyung; Choi, Seung-Ho; Choi, Jinwon; Lee, Jin Woo; Kang, Ki Sung; Shim, Sang Hee

doi:10.1016/j.bmcl.2023.129186

Bioorganic & Medicinal Chemistry Letters

2023

DOI: 10.1016/j.bmcl.2023.129186

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2,3-Dihydrosorbicillin and chrysopanol stimulate insulin secretion in INS-1 cells

Dahae Lee

Jae‐Kyung Kim

Seung-Ho Choi

et al.

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2024

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Cited by 2 publications

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Design, Synthesis and Computational Insight of Isolated and Thiophene fused 2H‐Pyran‐2‐ones as PPAR‐γ Agonist

Shah,

Nemaysh,

Althagafi

et al. 2024

ChemistrySelect

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Peroxisome proliferator‐activated receptor gamma (PPAR‐γ) is a well‐known member of the PPAR family and a potential target for the treatment of various disorders. Herein, we present the design and synthesis of various 6‐aryl‐4‐sec.amino‐2‐oxo‐2H‐pyran‐3‐carbonitrile derivatives and functionalized thieno[3,2‐c]pyran‐2‐ones, derived from ketene dithioacetal. Then all the synthesized compounds were docked for their activity as PPAR‐γ to predict the binding mechanism and affinities regarding rosiglitazone and muraglitazar. Our studies revealed that three compounds 10 e, 10 f, and 10 h showed significant binding affinities, with energy ranges comparable to standard drugs rosiglitazone and muraglitazar. The docking conformation studies revealed that the selected compounds nicely interact with PPAR‐γ in the ligand binding domain with positive predictive values. We also performed molecular dynamics of the most potent compounds to validate the result. Our results indicate that these novel compounds are potential PPAR‐γ ligands, offering new possibilities for therapeutic applications. This study underscores the potential of these synthesized compounds in the development of novel PPAR‐γ agonists.

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Design, Synthesis and Computational Insight of Isolated and Thiophene fused 2H‐Pyran‐2‐ones as PPAR‐γ Agonist

Shah,

Nemaysh,

Althagafi

et al. 2024

ChemistrySelect

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Targeted isolation of sorbicilinoids from a deep-sea derived fungus with anti-neuroinflammatory activities

Wu,

Meng,

Liu

et al. 2024

Phytochemistry

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2,3-Dihydrosorbicillin and chrysopanol stimulate insulin secretion in INS-1 cells

Cited by 2 publications

References 38 publications

Design, Synthesis and Computational Insight of Isolated and Thiophene fused 2H‐Pyran‐2‐ones as PPAR‐γ Agonist

Design, Synthesis and Computational Insight of Isolated and Thiophene fused 2H‐Pyran‐2‐ones as PPAR‐γ Agonist

Targeted isolation of sorbicilinoids from a deep-sea derived fungus with anti-neuroinflammatory activities

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