Background: As a new kind of green media and bioactive compounds with special
structure, Ionic Liquids (ILs) are attracting much attention and applied widely in many fields.
However, their roles and potential have not been fully recognized by many researchers of medicinal
chemistry. Because of obvious differences from other traditional drugs and reagents, their
uses and performance together with advantages and disadvantages need to be explored and reviewed
Methods: For a systematic and explicit description of the relationship between ILs and medicinal
chemistry, all of the contents were elucidated and summarized in a series of independent parts. In
each part, it started from the research background or a conceptual framework and then specific
examples were introduced to illustrate the theme. Finally, the important conclusions were drawn
and its future was outlooked after the discussion about related key problems appearing in each
mentioned research. Meanwhile, methodologies such as empirical analysis, comparison and induction
were applied in different sections to exposit our subject.
Results: The whole review was composed of five parts, and 148 papers were cited in total. Related
basic information of ionic liquids was provided on the basis of representative references,
including their concepts and important characters. Then 82 papers outlined ionic liquid-like active
pharmaceutical ingredients, which unfolded with their major biological activities (antimicrobial
activity, antibiofilm activity, antitumor activity, anticholinesterase activity and so on). Applications
of ionic liquids in the synthesis of drugs and pharmaceutical intermediates were elaborated
in 92 papers to illustrate the important roles of ILs and their extraordinary properties in this
field. Moreover, new technologies (such as immobilization of IL, microwave reaction, solventfree
synthesis, microreactor, etc) were introduced for further innovation. Finally, 26 papers were
included to expound the status of the IL-assisted derivatization of various natural lead compounds.
Conclusion: This review placed emphasis on chemical structures of ILs and their structureactivity
relationships in a specific manner, leading to meaningful and valuable related information
to some related fields and thus promotes further development and application of various ILs
for medicinal chemistry. The deep exploration for key scientific problems is the driving force to
propel their theoretical breakthrough and industrial production.