Fusion heterocyclic compounds have various biological activities, such as anticancer, antibacterial, antifungal and anti-inflammatory, and thus have been widely used in the field of medicinal chemistry. Pyrrolopyrimidines are a major class of fused heterocyclic compounds. Compared with single pyrrole and pyrimidine cores, pyrrolopyrimidines have more diverse and effective pharmacological characteristics as fusion scaffolds.
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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