{
  "abstract": "Background: Hyperlipidemia is a global health concern characterized by elevated blood lipid concentrations, including cholesterol and triglycerides. Cholesteryl ester transfer protein (CETP) plays a crucial role in transferring cholesteryl esters and phospholipids from antiatherogenic high-density lipoproteins to atherogenic low-density and very-low-density lipoproteins.\n\nObjectives: This study aimed to synthesize and evaluate 20 p-methoxy-substituted benzene sulfonamides (6a-6j and 7a-7j) as potential CETP inhibitors.\n\nMethods: The compounds were synthesized and structurally characterized using infrared (IR) spectroscopy, carbon-13 nuclear magnetic resonance (13C-NMR) spectroscopy, proton nuclear magnetic resonance (1H-NMR) spectroscopy, and high-resolution mass spectrometry, followed by evaluation of CETP inhibitory activity. Molecular modeling studies were also performed.\n\nResults: The biological assay showed that inhibitors 7f-7j exhibited the highest inhibitory activity, achieving 100% inhibition at 10 µM; inhibitor 7j had an IC50 of 0.55 µM. Compounds 6a-6j and 7a-7e showed CETP inhibition of up to 95%. The presence of an additional ring markedly enhanced activity, likely due to the hydrophobic nature of CETP. The docking results supported this finding, indicating that ligand/4EWS complex formation was driven by hydrophobic interactions and hydrogen-bond formation with the amino acid residues H232 and R201. Higher binding scores were observed for series 7a-7j than for series 6a-6j, highlighting the importance of introducing an additional ring to enhance CETP inhibition. Furthermore, pharmacophore mapping confirmed that these analogues matched the fingerprint of active CETP inhibitors.\n\nConclusions: A series of novel p-methoxybenzene sulfonamides was synthesized and evaluated as CETP inhibitors.",
  "abstract_shown": true,
  "affiliations": [
    "Faculty of Pharmacy, Al-Zaytoonah University of Jordan Amman Jordan"
  ],
  "article_type": "research article",
  "arxiv": null,
  "author_total": 5,
  "authors": [
    {
      "affs": [
        0
      ],
      "name": "Reema Abu Khalaf",
      "orcid": "0000-0002-7797-8918"
    },
    {
      "affs": [
        0
      ],
      "name": "Maha Awad",
      "orcid": "0000-0003-0530-6298"
    },
    {
      "affs": [
        0
      ],
      "name": "Mohammad Awad",
      "orcid": "0000-0003-1827-8775"
    },
    {
      "affs": [
        0
      ],
      "name": "Dima Sabbah",
      "orcid": "0000-0003-1428-5097"
    },
    {
      "affs": [
        0
      ],
      "name": "Ghadeer Albadawi",
      "orcid": "0000-0001-8323-8839"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/fxrhf1fre0z9n.bib",
  "cited_by": 0,
  "doi": "10.5812/ijpr-170876",
  "fulltext_url": "https://pmc.ncbi.nlm.nih.gov/articles/PMC13727966/",
  "id": "fxrhf1fre0z9n",
  "issns": [
    "1735-0328",
    "1726-6890"
  ],
  "landing_url": "https://doi.org/10.5812/ijpr-170876",
  "language": "en",
  "licence": "CC-BY-4.0",
  "licence_label": "CC BY 4.0",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "heading",
      "Research Article"
    ],
    [
      "openalex",
      "1605|Heterocyclic Compound Synthesis and Bioactivity"
    ]
  ],
  "openalex": "W7223568291",
  "pdf_url": "https://brieflands.com/journals/ijpr/articles/170876.pdf",
  "pmcid": "PMC13727966",
  "pmid": "42978991",
  "published": "2026-10-17",
  "publisher": "Brieflands",
  "ris": "https://research.draconitic.com/paper/fxrhf1fre0z9n.ris",
  "sources": [
    {
      "first_seen": "2026-11-06T12:23:44Z",
      "native_id": "PMC13727966",
      "source": "pmc",
      "url": "https://doi.org/10.5812/ijpr-170876"
    }
  ],
  "subjects": [
    {
      "field": "chemistry",
      "origin": "openalex:1605|Heterocyclic Compound Synthesis and Bioactivity",
      "subfield": "organic"
    }
  ],
  "title": "Design, Synthesis, and CETP Inhibitory Evaluation of Novel P-methoxybenzene Sulfonamides Supported by Molecular Modeling",
  "title_text": "Design, Synthesis, and CETP Inhibitory Evaluation of Novel P-methoxybenzene Sulfonamides Supported by Molecular Modeling",
  "type": "peer-reviewed",
  "updated_at": "2026-11-07T12:21:03Z",
  "url": "https://research.draconitic.com/paper/fxrhf1fre0z9n",
  "venue": "Iranian Journal of Pharmaceutical Research : IJPR",
  "versions": []
}