79338-42-4Relevant articles and documents
Isostearyl Mixed Anhydrides for the Preparation of N-Methylated Peptides Using C-Terminally Unprotected N-Methylamino Acids
Cary, Douglas R.,Handa, Michiharu,Kobayashi, Yutaka,Kurasaki, Haruaki,Masuya, Keiichi,Matsuda, Ayumu,Matsumoto, Masatoshi,Morimoto, Koki,Nagaya, Akihiro,Nishizawa, Naoki,Taguri, Tomonori,Takeuchi, Hisayuki
supporting information, p. 8039 - 8043 (2020/11/02)
Sustainable and efficient manufacturing methods for N-methylated peptides remain underexplored despite growing interest in therapeutic N-methylated peptides within the pharmaceutical industry. A methodology for the coupling of C-terminally unprotected N-methylamino acids mediated by an isostearic acid halide (ISTAX) and silylating reagent has been developed. This approach allows for the coupling of a wide variety of amino acids and peptides in high yields under mild conditions without the need for a C-terminal deprotection step in the process of C-terminal elongation. These advantages make this a useful synthetic method for the production of peptide therapeutics and diagnostics containing N-methylamino acids.
Synthesis and biological activity of a series of tetrasubstituted- imidazoles as P2X7 antagonists
Gleave, Robert J.,Walter, Daryl S.,Beswick, Paul J.,Fonfria, Elena,Michel, Anton D.,Roman, Shilina A.,Tang, Sac-Pham
scheme or table, p. 4951 - 4954 (2010/10/04)
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were investigated both with respect to activity at the P2X7 receptor and in vitro metabolic stability. Compound 10 was identified as a potent P2X7 antagonist with reduced in vitro metabolism and high solubility.
An efficient procedure for the preparation of Fmoc-amino acids
Raillard, Stephen P.,Mann, Adam D.,Baer, Ted A.
, p. 183 - 186 (2007/10/03)
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