By Antonio Guarna
A peptidomimetic is a small protein-like chain designed to imitate a peptide with adjusted molecular houses corresponding to superior balance or organic job. it's a very strong technique for the new release of small-molecule-based medicinal drugs as enzyme inhibitors or receptor ligands.
Peptidomimetics in natural and Medicinal Chemistry outlines the recommendations and artificial techniques underlying the construction of bioactive compounds of a peptidomimetic nature. subject matters lined contain the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, spine isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as flip inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case experiences within the hit-to-lead method, equivalent to the improvement of integrin ligands and thrombin inhibitors, illustrate the winning software of peptidomimetics in drug discovery.
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Extra info for Peptidomimetics in Organic and Medicinal Chemistry
Et al. (2003) Angew. , Int. , 42, 535. , Hong, S. et al. (2009) J. Am. Chem. , 131, 5564. Maity, P. and Koenig, B. (2008) Org. , 10, 1473. The Basics of Peptidomimetics 17 21. D. T. (1997) Annu. Rev. , 66, 385. 22. Moriuchi, T. and Hirao, T. (2004) Chem. Soc. , 33, 294. 23. , Mackin, G. et al. (1996) J. Am. Chem. , 118, 2764. D. and Maitra, S. (1999) J. Am. Chem. , 121, 8409. 24. S. R. , 29, 5081. 25. , Zabel, M. and König, B. (2004) Org. , 6, 1349. 26. (a) Feigel, M. (1986) J. Am. Chem. , 108, 181.
Finally, ether-bridged peptidomimetics have been developed for the construction of macrocyclic compounds. These have been approached by introducing bis-aryl ether bonds using SN Ar , copper-catalysed Ullman reaction  or aryl boronic acid-mediated cyclization , or by developing alkyl-aryl ether bonds by means of SN Ar  and intramolecular Mitsunobu reactions . This approach has been applied to achieve a tether between backbone moieties linked to side-chain functional groups, resulting in the corresponding cyclic compound.
More complex local modifications have considered the introduction of dipeptide isosteres, with aim of mimicking amide bond and side-chains with suitable chemical moieties. The dipeptide fragment is commonly addressed with cyclic compounds possessing chemical tethers for imposing restricted conformations. In addition, retro-inverso isomeric moieties, double bond fragments and cyclic cis-amide bond isosteres have been proposed with aim of replacing the amide bond without altering the topology of the adjacent side-chains of the corresponding dipeptide.