Imidazole is an important five-membered nitrogen-containing heterocyclic compound. Among the numerous heterocyclic compounds, imidazole and its derivatives are regarded as a unique and multifaceted scaffold material due to their diverse applications in industrial, organic and pharmaceutical chemistry. Imidazoles interact in different ways with many therapeutic targets, enzymes and receptors in biological systems and thus exhibit a wide range of biological activities. In particular, several imidazoles can be used as clinical drugs to treat various types of cancer with high therapeutic efficacy. Furthermore, imidazoles are one of the most critical segments in the field of anti-covid-19 virus drug discovery due to their ability to interact with active targets in living systems.
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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.
Thiadiazoles are a subfamily of azoles. Structurally, they are five-membered heterocyclic compounds containing two nitrogen atoms and one sulfur atom, and two double bonds, forming an aromatic ring. Depending on the relative positions of the heteroatoms, there are four possible structures; these forms do not interconvert and are therefore structural isomers rather than tautomers. These compounds themselves are rarely synthesized and have no particular utility, however, compounds that use them as structural motifs are fairly common in pharmacology.
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