The intrinsic role of heterocyclic compounds in medicinal chemistry is now undoubtful as more than 90% of new drugs contain heterocycles. Compounds possessing heterocyclic cores have several advantages that make their use in drug design particulary effective.
- Aromatic rings are extremely rigid in conformation thus defining spatial orientation of attached functional groups and reducing entropy of binding of the molecule with potential biological target.
- In most cases, hetero atoms exhibit properties of strong hydrogen bond donors/acceptors enforcing interaction of the molecule with its biological target.
- The chemistry of heterocyclic compounds is undoubtedly the most explored area of organic chemistry. The synthetic methods for the construction of heterocycles are well-established, simple, highly efficient and easy-scalable.
- Heterocycles occupy an overwhelming majority of the available chemical space thus being the most diverse class of organic compounds. Therefore they represent the substantial possibilities for the design of novel scaffolds that are yet not protected by patents.