Abstract
Oxindole derivatives 3-25 have been synthesized from commercially available oxindole by refluxing with different aromatic aldehydes in good yields. Their in vitro antiglycation potential has been evaluated. They showed a varying degree of antiglycation activity with IC50 values ranging between 150.4 - 856.7 µM. 3-[(3-Chlorophenyl)methylidene]- 1,3-dihydro-2H-indol-2-one (IC50 = 150.4 ± 2.5 µM) is the most active compound among the series, better than the standard rutin with an IC50 value 294.5 ± 1.50 µM. The structures of the compounds were elucidated by 1H-NMR and mass spectroscopy and elemental analysis. A limited structure-activity relationship has been developed.
Keywords: Oxindole, benzaldehydes, antiglycation, rutin, AGEPs.
Medicinal Chemistry
Title:Oxindole Derivatives: Synthesis and Antiglycation Activity
Volume: 9 Issue: 5
Author(s): Khalid Mohammed Khan, Momin Khan, Nida Ambreen, Muhammad Taha, Fazal Rahim, Saima Rasheed, Sumayya Saied, Humaira Shafi, Shahnaz Perveen and Muhammad Iqbal Choudhary
Affiliation:
Keywords: Oxindole, benzaldehydes, antiglycation, rutin, AGEPs.
Abstract: Oxindole derivatives 3-25 have been synthesized from commercially available oxindole by refluxing with different aromatic aldehydes in good yields. Their in vitro antiglycation potential has been evaluated. They showed a varying degree of antiglycation activity with IC50 values ranging between 150.4 - 856.7 µM. 3-[(3-Chlorophenyl)methylidene]- 1,3-dihydro-2H-indol-2-one (IC50 = 150.4 ± 2.5 µM) is the most active compound among the series, better than the standard rutin with an IC50 value 294.5 ± 1.50 µM. The structures of the compounds were elucidated by 1H-NMR and mass spectroscopy and elemental analysis. A limited structure-activity relationship has been developed.
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Cite this article as:
Khan Mohammed Khalid, Khan Momin, Ambreen Nida, Taha Muhammad, Rahim Fazal, Rasheed Saima, Saied Sumayya, Shafi Humaira, Perveen Shahnaz and Choudhary Iqbal Muhammad, Oxindole Derivatives: Synthesis and Antiglycation Activity, Medicinal Chemistry 2013; 9 (5) . https://dx.doi.org/10.2174/1573406411309050007
DOI https://dx.doi.org/10.2174/1573406411309050007 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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