Background: In recent years, the development and diversification of heterocyclic compounds has
become central to the discovery of bioactive compounds with novel or improved pharmacological properties.
In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received
huge attention of the medicinal chemists.
Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance.
Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent
drug candidates. The current review article described biological potential of various monocyclic azoles. Recent
developments in the synthesis of azole derivatives have been also reviewed.
Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics,
pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed
various biological activities and number of molecules are in clinical practice. A number of important leads and
potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple,
atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.