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New reagents, reactions, and peptidomimetics for drug design
Author(s) -
Goodman Murray,
Zapf Christoph,
Rew Yosup
Publication year - 2001
Publication title -
peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/1097-0282(2001)60:3<229::aid-bip10034>3.0.co;2-p
Subject(s) - peptidomimetic , chemistry , reagent , combinatorial chemistry , drug , organic chemistry , pharmacology , biochemistry , peptide , medicine
It has been a major focus in our laboratories to prepare novel reagents and peptidomimetic structures for drug design. We have designed and prepared novel guanidinylation reagents that can be employed in solution or as solid phase reagents. We and others have utilized the reagent 3‐(diethoxyphosphoryloxy)‐1,2,3‐benzotriazin‐4(3H)‐one (DEPBT) for amide bond formation to couple sterically hindered structures. These couplings proceed with remarkably strong resistance to racemization. In the area of peptidomimetics, we have incorporated novel building blocks to create biologically active compounds. These building blocks include thioether and alkylamine bridges, β‐methylated, and β,β‐dimethylated amino acid residues. These mimetic structures have been incorporated into specific target molecules such as opioids to obtain cyclic peptidomimetics with potent and selective biological activity. © 2001 John Wiley & Sons, Inc. Biopolymers (Pept Sci) 60: 229–245, 2001