2. Academic Validation
  3. Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

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

  • Eur J Med Chem. 2014 Sep 12:84:731-8. doi: 10.1016/j.ejmech.2014.07.078.
Muhammad Taha 1,  Nor Hadiani Ismail 2,  Waqas Jamil 3,  Hesham Rashwan 4,  Syed Muhammad Kashif 3,  Amyra Amat Sain 5,  Mohd Ilham Adenan 6,  El Hassane Anouar 7,  Muhammad Ali 8,  Fazal Rahim 9,  Khalid M Khan 10
Affiliations

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.
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.

Keywords

Antiglycation; Antileishmanial; Antioxidant; Benzimidazole; Stereoisomers.

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