Review article Therapeutic evolution of benzimidazole derivatives in the last quinquennial period Wasim Akhtar a , Mohemmed Faraz Khan a , Garima Verma a , M. Shaquiquzzaman a , M.A. Rizvi b , Syed Hassan Mehdi b , Mymoona Akhter a , M. Mumtaz Alam a, * a Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India b Department of Biosciences, Jamia Millia Islamia, New Delhi 110025, India article info Article history: Received 30 September 2016 Received in revised form 10 November 2016 Accepted 3 December 2016 Available online 5 December 2016 Keywords: Heterocyclic Benzimidazole Biological activity Anti-inflammatory and analgesic Anti-cancer Antiviral abstract Benzimidazole, a fused heterocycle bearing benzene and imidazole has gained considerable attention in the field of contemporary medicinal chemistry. The moiety is of substantial importance because of its wide array of pharmacological activities. This nitrogen containing heterocycle is a part of a number of therapeutically used agents. Moreover, a number of patents concerning this moiety in the last few years further highlight its worth. The present review covers the recent work published by scientists across the globe during last five years. © 2016 Published by Elsevier Masson SAS. Contents 1. Introduction ...................................................................................................................... 705 2. Pharmacological activities .......................................................................................................... 706 2.1. Anti-cancer activity .......................................................................................................... 708 2.2. Anti-inflammatory and analgesic activity .............................................. ........................................ 722 2.3. Anti-microbial activity ....................................................... ................................................ 725 2.4. Neuro-protective agents ...................................................... ............................................... 733 2.5. Anti-hypertensive agents ..................................................................................................... 736 2.6. Antiviral activity ............................................................................................................. 739 2.7. Anti-tubercular activity ....................................................................................................... 741 2.8. Anti-protozoal activity ........................................................................................................ 743 2.9. Miscellaneous ............................................................................................................... 743 3. Conclusion ....................................................................................................................... 746 References ........................................................................................................................ 746 1. Introduction The chemistry of benzimidazole (Fig. 1) has been an interesting field of study since decade. Benzimidazole is a moiety that contains benzene and a heterocyclic imidazole ring. It is one of the most promising moieties that is present in many clinically useful drugs * Corresponding author. E-mail address: drmmalam@gmail.com (M.M. Alam). Contents lists available at ScienceDirect European Journal of Medicinal Chemistry journal homepage: http://www.elsevier.com/locate/ejmech http://dx.doi.org/10.1016/j.ejmech.2016.12.010 0223-5234/© 2016 Published by Elsevier Masson SAS. European Journal of Medicinal Chemistry 126 (2017) 705e753