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DESIGN AND SYNTHESIS OF SOME NOVEL PEPTIDOMIMETIC SCAFFOLDS. Gagandeep Singh, Surinderjit S. Bhella, Mohan Paul S. Ishar

DESIGN AND SYNTHESIS OF SOME NOVEL PEPTIDOMIMETIC SCAFFOLDS.

Gagandeep Singh, Surinderjit S. Bhella, Mohan Paul S. Ishar


International Journal of Natural Product Science 2012: Spl Issue 1:101.

Abstract(RBIP-101)

Research on synthetic foldamers (peptidomimetics) has been attracting most attention not only for discovering predictable and well defined structures, but also on harnessing the latent bioactivities in enzyme mimics as well as drug design and drug development.1 For understanding the biologically relevant conformations of the molecules, the synthesis of conformationally constrained analogues is the most common approach employed and the same is achieved in case of peptides through insertion of conformationally constrained non-peptide scaffolds in the peptide backbone.2 As probes of both structural effects and properties, conformationally constrained cyclopropane derivatives have been widely employed as - and - turn mimics in peptidomimetics synthesis, such as constrained analogs of glutamic acid which are NMDA antagonists useful for treatment of chronic neuro-degenerative conditions like Alzheimer and Parkinsonism.3 We had reported the synthesis of turn inducer cyclopropane scaffolds.4 The present investigations were aimed at rational design, synthesis and understanding the influence of the introduction of some rigid scaffolds, such as cyclopropanes in peptide backbones, on the peptide conformation; the cyclopropane moiety can be further exploited as the chiral (inducer) scaffold.


Further pharmacological investigations will be carried out with the most active molecule for unraveling the mode of action along with target identification, which can be used for further designing.
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