183442-69-5Relevant academic research and scientific papers
A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids
Foley, Daniel J.,Doveston, Richard G.,Churcher, Ian,Nelson, Adam,Marsden, Stephen P.
supporting information, p. 11174 - 11177 (2015/07/07)
A powerful strategy for the efficient lead-oriented synthesis of novel molecular scaffolds is demonstrated. Twenty two scaffolds were prepared from just four α-amino acid-derived building blocks and a toolkit of six connective reactions. Importantly, each individual scaffold has the ability to specifically target lead-like chemical space.
The 'unexpected' epimerization on bicyclic thiazolidine γ-lactam scaffolds
Liu, Ruzhang,Wu, Yang,Li, Qiang,Liao, Wensheng,Chen, Shu-Hui,Li, Ge,Betancort, Juan M.,Winn, David T.,Campbell, David A.
, p. 4363 - 4369 (2008/09/21)
Preliminary findings related to the base induced cyclization and spontaneous epimerization leading to stereochemically defined bicyclic thiazolidine γ-lactam systems are reported.
The synthesis of β-strand mimetic templates via regioselective 1,3-dipolar cycloaddition with vinylsulfone
Fuchi, Nobuhiro,Doi, Takayuki,Harada, Takeo,Urban, Jan,Cao, Bolong,Kahn, Michael,Takahashi, Takashi
, p. 1305 - 1308 (2007/10/03)
We have developed a practical synthetic route to constrained β-strand mimetic templates by regioselective 1,3-dipolar cycloaddition of azomethine imines with vinyl sulfone. A small library of β-strand mimetic templates was generated which include potent and selective inhibitors of serine proteases.
Secondary structure peptide mimetics: Design, synthesis, and evaluation of β-strand mimetic thrombin inhibitors
Boatman, P. Douglas,Ogbu, Cyprian O.,Eguchi, Masakatsu,Kim, Hwa-Ok,Nakanishi, Hiroshi,Cao, Bolong,Shea, J. Paul,Kahn, Michael
, p. 1367 - 1375 (2007/10/03)
Constrained dipeptide mimetic templates were designed to mimic the secondary structure of peptides in a β-strand conformation. Two templates corresponding to the D-Phe-Pro portion of the thrombin inhibitor D-Phe-Pro- ArgCH2Cl were synthesized a
