Quinazolines belong to heterocyclic chemistry, also known as 1,3-naphthalenes. The backbone consists of two six-membered aromatic rings fused to each other, with two nitrogen atoms at positions 1 and 3 on the backbone. The presence of these two nitrogen atoms in quinazoline increases its importance in pharmaceutical and biological reactions. Quinazolines and their derivatives are among the most important heterocyclic compounds due to their diverse chemical reactivity and important range of biological activities.
Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
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