1. Academic Validation
  2. Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective

Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective

  • Eur J Med Chem. 2021 Jan 15:210:112994. doi: 10.1016/j.ejmech.2020.112994.
Om P S Patel 1 Omobolanle Janet Jesumoroti 2 Lesetja J Legoabe 3 Richard M Beteck 2
Affiliations

Affiliations

  • 1 Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address: 35568623@nwu.ac.za.
  • 2 Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
  • 3 Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address: lesetja.legoabe@nwu.ac.za.
Abstract

Nitroimidazoles based compounds remain a hot topic of research in medicinal chemistry due to their numerous biological activities. Moreover, many clinical candidates based on this chemical core have been reported to be valuable in the treatment of human diseases. Metronidazole (MTZ) derived conjugates demonstrated a potential application in medicinal chemistry research over the last decade. In this review, we summarize the synthesis, key structure-activity-relationship (SAR) and associated biological activities such as antimicrobial, Anticancer, antidiabetic, anti-inflammatory, anti-HIV and Anti-parasitic (Anti-trichomonas, antileishmanial, antiamoebic and anti-giardial) of explored MTZ-conjugates. The molecular docking analysis is also presented simultaneously, which will assist in developing an understanding towards designing of new MTZ-conjugates for target-based drug discovery against multiple disease areas.

Keywords

Biological activities; Metronidazole-conjugates; Molecular docking study; Nitroimidazole; Structure-activity relationship (SAR); Synthesis.

Figures