Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

Taha M 1 , Ismail NH 2 , Jamil W 3 , Rashwan H 4 , Kashif SM 3 , Sain AA 5 Show all authors , Adenan MI 6 , Anouar el H 7 , Ali M 8 , Rahim F 9 , Khan KM 10

Affiliations 

  • 1 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 43200 Puncak Alam, Selonger, Malaysia; Faculty of Applied Science UiTM, 40450 Shah Alam, Selangor D. E., Malaysia. Electronic address: taha_hej@yahoo.com
  • 2 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 43200 Puncak Alam, Selonger, Malaysia; Faculty of Applied Science UiTM, 40450 Shah Alam, Selangor D. E., Malaysia
  • 3 Institute of Advance Research Studies in Chemical Sciences, University of Sindh Jamshoro, Pakistan
  • 4 Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam 42300, Selangor, Malaysia
  • 5 Malaysian Institute of Pharmaceuticals and Nutraceuticals, Ministry of Science, Technology and Innovation, Bangunan Pentadbiran, Blok 5-A, Halaman Bukit Gambir,11700 Bayan Lepas, Penang, Malaysia
  • 6 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 43200 Puncak Alam, Selonger, Malaysia; Malaysian Institute of Pharmaceuticals and Nutraceuticals, Ministry of Science, Technology and Innovation, Bangunan Pentadbiran, Blok 5-A, Halaman Bukit Gambir,11700 Bayan Lepas, Penang, Malaysia; Forest Research Institute Malaysia (FRIM), 52109 Kepong, Selangor, Malaysia
  • 7 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 43200 Puncak Alam, Selonger, Malaysia
  • 8 Center for Advanced Drug Research, COMSATS Institute of Information Technology, University Road, Abbottabad 22060, KPK, Pakistan
  • 9 Department of Chemistry, Hazara University, Mansehra, Pakistan
  • 10 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
Eur J Med Chem, 2014 Sep 12;84:731-8.
PMID: 25069019 DOI: 10.1016/j.ejmech.2014.07.078

Abstract

4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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