- Alkali-metal hexamethyldisilazide initiated polymerization on alpha-amino acid N-substituted N-carboxyanhydrides for facile polypeptoid synthesis
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Polypeptoids have been explored as mimics of polypeptides, owing to polypeptoids’ superior stability upon proteolysis. Polypeptoids can be synthesized from one-pot ring-opening polymerization of amino acid N-substituted N-carboxyanhydrides (NNCAs). However, the speed of polymerization of NNCAs can be very slow, especially for NNCAs bearing a bulky N-substitution group. This hindered the exploration on polypeptoids with more diverse structures and functions. Therefore, it is in great need to develop advanced strategies that can accelerate the polymerization on inactive NNCAs. Hereby, we report that lithium/sodium/potassium hexamethyldisilazide (Li/Na/KHMDS) initiates a substantially faster polymerization on NNCAs than do commonly used amine initiators, especially for NNCAs with bulky N-substitution group. This fast NNCA polymerization will increase the structure diversity and application of polypeptoids as synthetic mimics of polypeptides.
- Wu, Yueming,Zhou, Min,Chen, Kang,Chen, Sheng,Xiao, Ximian,Ji, Zhemin,Zou, Jingcheng,Liu, Runhui
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supporting information
p. 1675 - 1678
(2021/03/15)
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- DIPEPTIDYL PEPTIDASE INHIBITORS
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The present invention relates to novel inhibitors of serine type peptidases in general and of serine type dipeptidyl peptidases in particular. The present invention further relates to the use of the dipeptidyl peptidase inhibitors for selective inhibition
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Page 76; Figure 3
(2010/02/08)
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- BRADYKININ ANTAGONIST PEPTIDES INCORPORATING N-SUBSTITUTED GLYCINES
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The present invention provides bradykinin type peptides containing N-substituted glycines, particularly bradykinin antagonist peptides useful for the treatment of conditions mediated by bradykinin including pain and inflammation.
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- Bradykinin receptor antagonists containing N-substituted amino acids: In vitro and in vivo B2 and B1 receptor antagonist activity
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We report a systematic probing of the structural requirements of the bradykinin (BK) type 2 (B2) receptor for antagonist activity by incorporating N-alkyl-amino acid residues at positions 7 and 8 of a potent antagonist sequence. Compound 1 (D-A
- Goodfellow, Val S.,Marathe, Manoj V.,Kuhlman, Karen G.,Fitzpatrick, Timothy D.,Cuadrado, David,Hanson, Wendy,Zuzack, John S.,Ross, Sherman E.,Wieczorek, Maciej,Burkard, Michael,Whalley, Eric T.
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p. 1472 - 1484
(2007/10/03)
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