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Peptidic Macrocycles


    Peptidomimetic compound libraries play a pivotal role in the discovery ofnew molecules with high activity, specificity, and affinity against many therapeutically relevant targets. Synthetic analogs of natural peptides can effectively mimic the structural elements of natural ligands and produce the desired biological effect but further efforts are required to address metabolic challenges such as resistance to peptidases and permeability. Several studies suggest that the macrocyclization of peptidomimetics is an attractive strategy to improve important biological properties. Macrocyclic peptidomimetic compound libraries would, therefore,be a useful starting point in drug discovery. ASINEX has been continuously improving the design of macrocyclic compounds that can effectively mimic biologically relevant di- and tripeptide motifs which can serve as topological mimics of the secondary structuresof peptides (e.g.: alpha helixes, beta turns). Our approach is based on the synthesis of conformationally constrained, macrocyclic cores that typically contain 2-4 cyclic amide groups, along with several additional points of diversity which are used for the introduction of lipophilic or hydrophilic side chains. At ASINEX, the synthesis of macrocyclic compounds was carried out using two fundamental strategies: a macrolactamization approach of an amino acid precursor and a ring-closing metathesis (RCM) of a bis-olefin precursors. Our peptidic macrocycles tend to be larger than our scaffold-based non-peptidic macrocycles, yet many compounds demonstrate favorable aqueous solubility and membrane permeability as measured by PAMPA and Caco-2 assays.

Product Name: Format/Size Descriptions Download
Peptidomimetics 9144 compounds
For cherry-picking
Update: 2020-07
The file contains all available Peptidomimetics selected from our Signature & BioDesign Libraries.
SL#018
Spiro Peptidomimetics
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has developed several peptidomimetic scaffolds containing beta-amino acid and amino alcohol fragments integrated into a rigid spiro core. These cores have been decorated with various natural and unnatural amino acids resulting in a diverse library of tri-peptide mimetics.
SL#034
Macrocyclic β-turn mimetics
80 compounds
Pre-Plated Set
Release: 2016
Asinex has created a library of partially peptidic macrocyclic beta-turn mimetics that are able to reproduce the orientation of key amino-acid side chains forming a b-turn-like motif.
SL#040
Constrained Tetrapeptides
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a library of constrained tetrapeptides using a novel unnatural piperidine-containing amino acid fragment. The intrinsic rigidity from the piperidine ring is enhanced by judicial choice of other amino acids carefully decorated with diverse side chains. According to in-silico modeling some molecules can adopt a beta-turn-like conformation and can therefore be considered beta-turn mimetics.

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Product Name: Format/Size Descriptions Download
SL#059, 060
Oxo-SpiroPyrrolidines
80 compounds x 2
Pre-Plated Set
Release: 2016
ASINEX has developed a versatile synthetic approach to skeletally diverse novel spiro scaffolds that are based on a rare combination of O- and N-containing cycles with additional synthetic handles. This allows the introduction of various peripheral fragments which, in turn, create derivatives with a very attractive physico-chemical profile.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

N.Chestnut St., Ste.104

Winston-Salem, NC 27101

USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

Klaprozenweg 75C, 1033NN

Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

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