Download e-book for iPad: Advances in Amino Acid Mimetics and Peptidomimetics, Volume by A. Abell
By A. Abell
Peptidomimetics have came upon large program as bioavailable, and infrequently powerful mimetics of typical peptides. They shape the root of vital periods of enzyme inhibitors, they act as receptor agonists and antagonists, they usually have even been used to imitate DNA constitution. contemporary advances within the use of solid-phase natural synthesis have lead the way for the practise of libraries of those constructions to permit the fast optimization of theri organic homes and for this reason healing capability. we're additionally commencing to achieve a better figuring out of the structural good points of this classification of compounds that impression their skill to permeate membranes, and their price of clearance and metabolism. This quantity brings jointly a lot of those serious matters by means of highlighting fresh advances in a few middle peptidomimetic-based study.
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Additional resources for Advances in Amino Acid Mimetics and Peptidomimetics, Volume 2, Volume 2 (Advances in Amino Acid Mimetics and Peptidomimetics) (Advances in Amino Acid Mimetics and Peptidomimetics)
1998, 8, 2339.
Coupling of the unnatural amino acid building blocks, Fmoc-deprotection, acetylation and TFA cleavage yielded libraries which were screened for binding activity at the vitronectin receptor. Two of these libraries possessed significant inhibition (>50%) at 100 I~M. Truncation of the amino acid chains was used to optimize the potency of these libraries, leading to the discovery of inhibitors 123 and 124 (Figure 7). The authors note that since the potency of these compounds is much lower than existing antagonists, these structures were not optimized further.
O Boc--N n 170 /__CONHR1 Boc-N 0 ..... O ~(NHR 2 172 = O 1) HCl . . O RIHNOC'~"N"~X"~N/~CONHR1 . , R2HNOC') 173 Scheme 46. The Boger synthesis of trimerized iminodiacetic acid diamides. should allow for the mimicry of the GIy-X function. Extension of the 1 and 3 positions allows for a mirroring of the conformation of an extended sheet. In a representative example, simple ring opening of the anhydride 167 by amines afforded the mono-amide, which can be further transformed to the differentially substituted bis-amide 168.
Advances in Amino Acid Mimetics and Peptidomimetics, Volume 2, Volume 2 (Advances in Amino Acid Mimetics and Peptidomimetics) (Advances in Amino Acid Mimetics and Peptidomimetics) by A. Abell