Building units for N-backbone cyclic peptides. 1. Synthesis of protected N-(.omega.-aminoalkylene)amino acids and their incorporation into dipeptide units
摘要:
A variety of new amino acids which contain an omega-aminoalkylene group on the N(alpha)-amino nitrogen were synthesized by alkylation of alkylenediamines with alpha-halogeno acids. The reaction proceeds with inversion of configuration; thus, optically pure products were obtained when optically active a-halogeno acids were used. The N-(omega-aminoalkylene)amino acids were protected by orthogonal protecting groups to allow their incorporation into dipeptides by the "solution" techniques and into peptides by the solid-phase peptide synthesis (SPPS) methodology. A series of dipeptide analogs of Phe-Gly, Leu-Gly, Trp-Gly, Phe-Leu, and Phe-Ala in which the nitrogen of the peptide bond is alkylated by omega-aminoalkylene chains with various lengths were prepared. These new protected N-(omega-aminoalkylene)amino acids and their derived dipeptide units may be used as building blocks for conformationally constrained N-backbone cyclic peptides.
Building units for N-backbone cyclic peptides. 1. Synthesis of protected N-(.omega.-aminoalkylene)amino acids and their incorporation into dipeptide units
摘要:
A variety of new amino acids which contain an omega-aminoalkylene group on the N(alpha)-amino nitrogen were synthesized by alkylation of alkylenediamines with alpha-halogeno acids. The reaction proceeds with inversion of configuration; thus, optically pure products were obtained when optically active a-halogeno acids were used. The N-(omega-aminoalkylene)amino acids were protected by orthogonal protecting groups to allow their incorporation into dipeptides by the "solution" techniques and into peptides by the solid-phase peptide synthesis (SPPS) methodology. A series of dipeptide analogs of Phe-Gly, Leu-Gly, Trp-Gly, Phe-Leu, and Phe-Ala in which the nitrogen of the peptide bond is alkylated by omega-aminoalkylene chains with various lengths were prepared. These new protected N-(omega-aminoalkylene)amino acids and their derived dipeptide units may be used as building blocks for conformationally constrained N-backbone cyclic peptides.
To provide a novel diamine, and a polyimide precursor and a polyimide using it. A diamine represented by the formula (1):
wherein each of X
1
and X
5
which are independent of each other, is a single bond or the like; each of X
2
and X
4
which are independent of each other, is —CH
2
— or the like; X
3
is a C
1-6
alkylene or the like; each of Y
1
and Y
2
which are independent of each other, is a single bond or the like; R is a C
1-20
linear, branched or cyclic hydrocarbon group; and a is 0 or 1).
[EN] CYCLIC PEPTOID OLIGOMERS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME<br/>[FR] OLIGOMÈRES PEPTOÏDES CYCLIQUES, COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT ET PROCÉDÉS D'UTILISATION ASSOCIÉS
申请人:UNIV NEW YORK
公开号:WO2014159937A1
公开(公告)日:2014-10-02
Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: wherein R1 and n are as described herein. The peptoids demonstrate antimicrobial and antimalarial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial or malarial infection is involved. The present cyclic peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.
The invention is directed to analogs of LHRH-II and, more generally, to analogs of the LHRH family in which modifications have been made that confer enhanced binding affinity for LHRH receptors and/or improved metabolic stability.
The invention is further directed to methods of targeted therapy and targeted imaging in patients with sex-hormone-related cancers or other LHRH-mediated diseases.
To provide a novel diamine, and a polyimide precursor and a polyimide using it. A diamine represented by the formula (1):
wherein each of X1 and X5 which are independent of each other, is a single bond or the like; each of X2 and X4 which are independent of each other, is —CH2— or the like; X3 is a C1-6 alkylene or the like; each of Y1 and Y2 which are independent of each other, is a single bond or the like; R is a C1-20 linear, branched or cyclic hydrocarbon group; and a is 0 or 1).