Building Blocks

Timonacic is an analog of nicotinamide that has been shown to be an effective inhibitor of energy metabolism in the mitochondria. It has antioxidative properties and can protect against the development of heart disease by inhibiting the production of reactive oxygen species. Timonacic's anti-inflammatory properties may be due to its ability to inhibit prostaglandin synthesis. It also has a high affinity for fatty acids, which may contribute to its inhibitory effects on lipid peroxidation. This drug has a carboxy terminal and is used as a sodium salt, which may play a role in its enzyme inhibition activity. Timonacic inhibits the activities of enzymes such as carnitine acetyltransferase and pyruvate dehydrogenase kinase, which are involved in the biosynthesis of fatty acids. The intramolecular hydrogen bonds formed with timonacic may contribute to its inhibitory effect on these enzymes.

Bromo-PEG4-azide is a PEG compound with two different functional groups (also known as heterobifunctional). Unlike homobifunctional PEG compounds (same functional group on both ends), this type of compounds are more versatile as have two different anchor points. Bromo-PEG4-azide is used as a linker and spacer to add a PEG moiety, via pegylation (a bioconjugation technique) to proteins, peptides, oligonucleotides, small molecules and nanoparticles.

Methyl 5-hexynoate is a synthetic product that can be synthesized from soybean lipoxygenase and hydrogenation reduction. This product has been shown to be a useful synthon for the synthesis of monoclonal antibodies with high binding affinity. The synthetic pathway, which involves cross-coupling and asymmetric synthesis, is outlined in the diagram below. The following are the steps involved in the production of methyl 5-hexynoate: 1) Addition of ethyl bromide to terminal alkynes 2) Addition of hydrochloric acid 3) Reaction with potassium tert-butoxide 4) Hydrogenation reduction 5) Cross-coupling reaction 6) Asymmetric synthesis