Macrocyclic compounds are highly significant in drug and research development. When developing new drugs, macrocyclic compound are commonly researched in the medical field. Macrocyclic compounds are becoming more successfully recognised as an approach for low drug availability targets, such as antimicrobial, antiviral, and protein-protein interactions (PPIs). Topologically, macrocyclic compounds have a unique ability to span large surface areas whilst remaining conformationally restricted when compared to acyclic molecules of equivalent molecular weight. Macrocyclic compounds also reduce the overall polarity and enhance membrane permeability. Therefore, together these attributes make macrocycles a powerful approach for any lead discovery programme against challenging targets.

Research into macrocyclic compounds is increasing and are widely used in antibacterial, antiviral, and antitumor drugs for clinical applications. On antibacterial aspects, macrolides, cyclic peptides, aza-macrocyclic compounds, etc., for example, have the characteristics of broad antibacterial spectrum antibiotics. They also exhibit strong antibacterial activity, remarkable curative effect and circumvent drug resistance.

Clinical application of anti-herpes virus drugs, like ganciclovir and cidofovir have severe side effects with poor antiviral activity. Presently, attention is focused on research of naphthyridines. Some compounds already synthesised via computer technology are already exhibiting strong anti-herpes virus activity.

On anti-tumour aspects, epothilone has a similar mechanism of action as paclitaxel. Epothilone is highly toxic to cells that have developed resistance to paclitaxel, therefore overcomes the weakness displayed by paclitaxel.

With the continuous development of chemical synthesis technology, the discovery of macrocyclic lead compounds from natural products, improvement of the availability of genomic sequences and bioinformatics have marked the arrival of times of the exploration of new macrocyclic drugs. As research progresses macrocyclic drugs are sure to have a bright application prospect.

TargetMol’s Macrocyclic Compound Library collects 210 macrocyclic compounds of known activity for the study of macrocyclic drugs.