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Macrocyclic Library
 
Home > Libraries > Minimalist Libraries > Macrocyclic Library
 

Macrocyclic Library

 

ASINEX's Macrocyclic Compound Library

Under-represented structural class in screening collections

Mid-sized and large-sized ring compounds have always been considered by medicinal chemists as a stand-alone class of molecules, not only due to their interesting physico-chemical and biological properties, but also due to the challenge of their synthesis [1]. To address this issue, ASINEX has elaborated a medchem library of 5000 compounds in which a peptidomimetic macrocycle ring is attached to a privileged pharmacophore - piperidine, pyrrolidine etc. The resulting combination is novel and allows the generation of a tremendous diversity of medchem-relevant macrocyclic frameworks. The presence of intrinsic points of diversity allows for the introduction of additional pharmacophores into the periphery, which have been selected based on the analysis of known drugs and natural products.

Considering that macrocylic molecules tend to be larger and more lipohilic than traditional screening molecules, it is vital to control their physico-chemical properties in advance. Therefore all macrocyclic molecules have been tested for aqueous and DMSO solubility with the cut-offs of 10 mM in DMSO and 100 µM in PBS (pH 7.4). The synthesis strategy is based on ASINEX's expertise in olefin transformations and catalytic cyclizations.

Due to a restricted conformational flexibility and a favorable orientation of the exiting peripheral substituents, some of the macrocyclic compounds can effectively mimic the alpha helical or beta strand/sheet topology of some biologically relevant proteins.

Macrocyclic Library

The Macrocyclic Compound Library provides a very rich source of peptidomimetics and is ideal for probing challenging target classes including:

  • Protein-protein interactions
  • Antibacterial / antiviral targets

Library specifics
Measured Solubility: 100% of compounds are soluble in DMSO at 10 mM, and in PBS at 100 µM
Quality: min.purity of 90%, avg. of 95% (LC-MS, NMR), stored as dry powder

ASINEX's Macrocyclic Compound Library is only available upon request, please contact us at:
Tel.: +7 (495) 780 34 15, +7 (495) 780 34 10
E-mail : LSadovenko@asinex.com or Busdev@asinex.com


1. Lisa A. Marcaurelle et al. An Aldol-Based Build/Couple/Pair Strategy for the Synthesis of Medium- and Large-Sized Rings: Discovery of Macrocyclic Histone Deacetylase Inhibitors, J. Am. Chem. Soc., 2010, 132 (47), pp 16962-16976.

 
 
 
 
 
 
 
 
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