By Wieslaw M. Kazmierski
A cutting-edge choice of precise man made methods that result in numerous scaffolds, flip mimetics, peptide-bound replacements, and enzyme inhibitors. issues diversity from strange syntheses of amino acids to using quite a few linear and heterocyclic scaffolds in preference to the peptide spine. very important chemical techniques and techniques contain the temporary safeguard of charged peptides as impartial prodrugs for enhanced blood-brain penetration and the substitute of peptide bonds with heterocyclic earrings, olefins and fluoroolefins, and ketomethylenes. artificial protocols in the direction of the transition-state mimics and reactive "warheads," appropriate in enzyme inhibitors, also are disclosed.
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A state of the art choice of distinct man made systems that bring about numerous scaffolds, flip mimetics, peptide-bound replacements, and enzyme inhibitors. themes diversity from strange syntheses of amino acids to using quite a few linear and heterocyclic scaffolds instead of the peptide spine.
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2. Solid Phase Approach to the Synthesis of the Cyclic Prodrug 77 (Fig. 7. Synthesis of the Linear Peptide 15 A typical synthesis uses Wang’s alkoxy resin (Bachem Btoscience) (14) Fmoc protected ammo acids were used for the solid phase peptide synthesis unless otherwise indicated (15). The couplmg of the first ammo acid (p-benzyl-asparttc actd) requires direct acttvation of the carboxyl groups with DIC for optimal yields The couplmg of subsequent ammo acids used the DIC/HOBt method, and the reaction was monitored by the nmhydrm test (161, as well as by the weight of the resin The final cleavage of the peptide from the resin was accomplished by treatment with 50% TFA/DCM.
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