Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines are known to be the backbone of many bulk compounds and important core structures for approved drugs; studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity.
Quinolines are an important class of biologically active heterocyclic compounds, and their derivatives usually exhibit a variety of biological activities. They can be used as antimalarial drugs and in the preparation of other antimalarial drugs. Other important activities of quinoline derivatives include inhibitory activity against EGFR-TK and antipsychotic activity. Futhermore, quinoline scaffolds are present in various drug molecules, including the antimalarial drugs aablaquine, chloroquine, mefloquine and primaquine, and the antibacterial agents gatifloxacin, levofloxacin, and moxifloxacin.
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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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