By Antonio Guarna

ISBN-10: 1119950600

ISBN-13: 9781119950608

A peptidomimetic is a small protein-like chain designed to imitate a peptide with adjusted molecular houses comparable to more advantageous balance or organic task. it's a very robust process for the new release of small-molecule-based medications as enzyme inhibitors or receptor ligands.

Peptidomimetics in natural and Medicinal Chemistry outlines the techniques and artificial recommendations underlying the development 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 procedure, similar to the improvement of integrin ligands and thrombin inhibitors, illustrate the winning software of peptidomimetics in drug discovery.

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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. B. and Feigel, M. (1994) Helv. Chim. Acta, 77, 70.

2 Thrombin Inhibitors Among novel approaches to the treatment of thrombosis, since the 1980s major efforts have been devoted to the development of thrombin inhibitors. Thrombin is a trypsin-like serine protease formed through the cleavage of prothrombin by the serine protease factor Xa. 8 Peptidomimetic ACE inhibitor drugs fibrinolysis. It catalyses the conversion of fibrinogen into fibrin by cleaving the peptide bond between arginine and glycine in the fibrinogen sequence Gly-Val-Arg-Gly-Pro-Arg.

Mono- and multiple-N-methylations of cyclic peptides were investigated to elucidate their remarkable conformational modulation ability by imparting steric constraints in the peptidic backbone and in improving the pharmacokinetic profile of the peptides to be used as drug leads. In this respect, N-methylation introduces another dimension to this ‘spatial screening’ [14] due to the remarkable property of conformational modulation. In fact, N-methylation Synthetic Approaches towards Peptidomimetic Design 31 facilitates the occurrence of a cis-peptide bond and allows us to study the role of amide protons in establishing potential hydrogen bonds, resulting in optimization of the conformational and structural profile of a peptidomimetic.

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Peptidomimetics in Organic and Medicinal Chemistry by Antonio Guarna

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