Synthesis of glycophospholipid and peptide-phospholipid conjugat

Details Synthesis of glycophospholipid and peptide-phospholipid conjugat Synthesis of glycophospholipid and peptide-phospholipid conjugat

1996-10-15

2000-06-06

Kishore, Gollamudi S.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

436829, 514 2, 514 8, 514 21, 514 23, 514 53, 514 54, 530402, 530810, 536 261, 536120, 554 79, 935 54, A61K 9127, A61K 3800, C07H 1904, C07F 902

Patent

active

060715324

ABSTRACT:
The present invention provides glycophospholipid and peptide-phospholipid conjugates comprising a phospholipid moiety and a saccharide or peptide moiety joined by an ether linkage comprising a secondary or tertiary amine. The conjugate structure of the invention comprises a flexible spacer arm between the phospholipid and saccharide or peptide moieties which, being variable in length, serves to optimize saccharide or peptide bioactivity. This invention further provides a method for the synthesis of such conjugates comprising the step of reductive amination. The method is efficient, economical and provides a high yield of product. Glycophospholipid and peptide-phospholipid conjugates of the invention can be incorporated and, optionally, chemically polymerized in self-assembling systems such as membranes, bilayers, films, liposomes and the like, and find utility diagnostically and therapeutically in medical and immuno-biological applications.

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