What Are Macrocycles?
Macrocycles are generally described as molecules and ions containing twelve- or more-membered rings. Macrocyclic compounds describe a large and mature field of chemistry. The macrocycle often binds ions and facilitates the transport of ions across the hydrophobic membrane and solvent. It wraps the ions with a hydrophobic sheath, which facilitates the phase transfer characteristics.
What Are Macrocyclic Effects?
The macrocyclic effect is when the multidentate ligand forms a ring with the central metal atom or ion, since it is a multidentate ligand, the stability of the complex is enhanced. The macrocyclic effect is the high affinity of metal cations for macrocyclic ligands compared to their acyclic analogs.
What Is a Macrocyclic Ligand?
In chemistry, a macrocyclic ligand is a macrocyclic ring with a ring size of at least nine (including all heteroatoms) or more donor sites. Typical examples are crown ethers and porphyrins. Macrocyclic ligands show particularly high affinity for metal ions.
Why Macrocycles Used in Drug Discovery?
Macrocycles are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, improved pharmacokinetics for relatively large small-molecules, and for peptides.
Natural product macrocycles and their synthetic derivatives have long been clinically useful and attention is now being focused on the wider use of macrocyclic scaffolds in medicinal chemistry in the search for new drugs for increasingly challenging targets. With the increasing awareness of concepts of drug-likeness and the dangers of “molecular obesity”, functionalized macrocyclic scaffolds could provide a way to generate ligand-efficient molecules with enhanced properties.
What Are Macrocyclic Ligands Examples?
There are several classes of macrocyclic ligands, such as saturated polyazamacrocycles, imine Schiff-base macrocycles, oxazolidine-containing macrocycles, polyoxamacrocycles, polyoxaazamacrocycles, polyoxa- and oxaazacoronands, crown ethers, lariat crown ethers, cryptands, cavitands, calixarenes, and carcerands.
Where to Find Macrocycles?
Specializing in a range of formulation and drug delivery technologies, CD Bioparticles offers a series of macrocycles for research applications. Products such as (13)aneN4, 1,7-Diaza-12-crown-4, Cross-bridged-Cyclam (CB-Cyclam), CYCLAM, CYCLEN, TACD, TACN and TACN-3HCl are all available at CD Bioparticles. In addition, CD Bioparticles offers a list of chelating agents for scientific community, such as DFO Derivatives, TACN Derivatives, NOTA Derivatives, DTPA Derivatives, DOTA Derivatives, CYCLEN Derivatives, and CYCLAM Derivatives. We have strong and broad expertise and over years of experience in the drug delivery field. Any requirements about our macrocycles can be fulfilled at CD Bioparticles.
References
- Vendeville, Sandrine, et al. Synthetic macrocycles in small-molecule drug discovery. Annual Reports in Medicinal Chemistry. 2013, 371-386.
- Peterson, M. L. The Evolution of Macrocycles in Drug Discovery: from Technologies to Drugs. Pharma. Rev. 2017, 343609.
- Mallinson, Jamie, et al. Macrocycles in new drug discovery. Future medicinal chemistry. 2012, 1409-1438.