Abstract
A series of metronidazole ester derivatives 1-34 has been synthesized with the aim of developing new leads with antiglycation activity. The in vitro evaluation of antiglycation potential of 1-34 showed that the ester derivatives 28, 16, and 3 have IC50 values 218.97 ± 2.5, 245.3 ± 5.1, and 278.6 ± 0.8 μM, respectively, comparable to the standard agent, rutin (IC50 = 294.5 ± 1.50 μM). The study identifies a new class of potent antiglycation agents. A structure-activity relationship has also been evaluated. All the compounds were characterized by using spectroscopic techniques, including 1H NMR, IR, and EI-MS.
Keywords: AGE, Bovin serum albumin, Protein glycation, Inhibitors, Metronidazole, Ester derivatives, spectroscopic, NMR, Schiff bases, antifungal
Medicinal Chemistry
Title:Metronidazole Esters: A New Class of Antiglycation Agents
Volume: 8 Issue: 5
Author(s): Aurang Zeb, Imran Malik, Saima Rasheed, Muhammad Iqbal Choudhary and Fatima Z. Basha
Affiliation:
Keywords: AGE, Bovin serum albumin, Protein glycation, Inhibitors, Metronidazole, Ester derivatives, spectroscopic, NMR, Schiff bases, antifungal
Abstract: A series of metronidazole ester derivatives 1-34 has been synthesized with the aim of developing new leads with antiglycation activity. The in vitro evaluation of antiglycation potential of 1-34 showed that the ester derivatives 28, 16, and 3 have IC50 values 218.97 ± 2.5, 245.3 ± 5.1, and 278.6 ± 0.8 μM, respectively, comparable to the standard agent, rutin (IC50 = 294.5 ± 1.50 μM). The study identifies a new class of potent antiglycation agents. A structure-activity relationship has also been evaluated. All the compounds were characterized by using spectroscopic techniques, including 1H NMR, IR, and EI-MS.
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Cite this article as:
Zeb Aurang, Malik Imran, Rasheed Saima, Iqbal Choudhary Muhammad and Z. Basha Fatima, Metronidazole Esters: A New Class of Antiglycation Agents, Medicinal Chemistry 2012; 8 (5) . https://dx.doi.org/10.2174/157340612802084360
DOI https://dx.doi.org/10.2174/157340612802084360 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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