Medicinal Chemistry Research

, Volume 23, Issue 10, pp 4447–4454 | Cite as

2-(2′-Pyridyl) benzimidazole derivatives and their urease inhibitory activity

  • Zafar Saeed Saify
  • Arfa Kamil
  • Shamim Akhtar
  • Muhammad Taha
  • Ajmal Khan
  • Khalid Mohammed KhanEmail author
  • Sarwat Jahan
  • Fazal Rahim
  • Shahnaz Perveen
  • M. Iqbal Choudhary
Original Research


Pyridyl-benzimidazole analogues 111 with variable substituent on phenyl ring of phenacyl moiety were synthesized and evaluated for their urease inhibitory activity. The compounds exhibited urease inhibition with IC50 between 19.22 and 77.31 µM. Compounds 4 (IC50 = 19.22 ± 0.49 µM) showed a urease inhibition comparable to thiourea (IC50 = 21.00 ± 0.01 µM) and twofold more active than acetohydroxamic acid (IC50 = 42.00 ± 1.26 µM) (standards), respectively. Moreover, compounds 5 (IC50 = 21.55 ± 0.36 µM), 1 (IC50 = 24.37 ± 0.41 µM), 7 (IC50 = 25.44 ± 0.19 µM), 6 (IC50 = 27.62 ± 0.25 µM), 3 (IC50 = 31.32 ± 0.75 µM), 8 (40.88 ± 0.36 µM) and 9 (41.22 ± 0.42 µM) also exhibited excellent activities when compared to the standards. Compounds 2 (IC50 = 65.46 ± 0.75 µM), 10 (68.99 ± 0.33 µM) and 11 (77.31 ± 0.51 µM) showed a moderate activity. The size of the substituents and their electron donating or withdrawing affects as well as their position on phenyl apparently modulates the enzyme inhibitory activity.


Pyridyl-benzimidazole analogues Urease inhibition SAR Peptic ulcer 



The authors are thankful to the OPCW, The Netherlands, for their financial support for Project No. L/ICA/ICB/173681/12.


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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  • Zafar Saeed Saify
    • 1
  • Arfa Kamil
    • 2
  • Shamim Akhtar
    • 3
  • Muhammad Taha
    • 4
    • 5
  • Ajmal Khan
    • 1
  • Khalid Mohammed Khan
    • 1
    Email author
  • Sarwat Jahan
    • 2
  • Fazal Rahim
    • 6
  • Shahnaz Perveen
    • 7
  • M. Iqbal Choudhary
    • 1
    • 8
  1. 1.International Center for Chemical and Biological Sciences, H. E. J. Research Institute of ChemistryUniversity of KarachiKarachiPakistan
  2. 2.Department of Pharmaceutical ChemistryFederal Urdu University of Arts, Science and TechnologyKarachiPakistan
  3. 3.Department of Pharmaceutical ChemistryUniversity of KarachiKarachiPakistan
  4. 4.Atta-ur-Rahman Institute for Natural Product DiscoveryUniversiti Teknologi MARA (UiTM)Bandar Puncak AlamMalaysia
  5. 5.Faculty of Applied ScienceUniversiti Teknologi MARAShah AlamMalaysia
  6. 6.Department of ChemistryHazara UniversityMansehraPakistan
  7. 7.PCSIR Laboratories Complex, Shahrah-e-Dr. Salimuzzaman SiddiquiKarachiPakistan
  8. 8.Department of Biochemistry, Faculty of ScienceKing Abdul-Aziz UniversityJeddahSaudi Arabia

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