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.
Isoxazole is a liquid heterocyclic compound C3H3NO isomeric with oxazole and having a penetrating odor like that of pyridine. Isoxazoles belong to an important class of five-membered aromatic heterocycles containing two electronegative heteroatoms, nitrogen and oxygen, in a 1,2-relationship and three regular sp2 carbon atoms. These molecules are found to be key components in various synthetic products in daily use and also present as a pharmacophore essential for biological activity in many drugs and bioactive natural products. In addition, isoxazoles have demonstrated their ability to exhibit hydrogen bond donor/acceptor interactions with a variety of enzymes and receptors.
Oxazoles are heterocyclic aromatic compounds containing one oxygen atom and one nitrogen atom, separated by a carbon atom. The presence of two heteroatoms (oxygen and nitrogen) provides possible interactions (hydrogen, hydrophobic, van der Waals or dipole bonds) with a wide range of receptors and enzymes. Oxazole rings are valuable heterocyclic scaffolds for the design of novel therapeutics with anticancer, antiviral, antibacterial, anti-inflammatory, neuroprotective, antidiabetic, and antidepressant properties due to their wide range of targets and biological activities.
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