Cyclic peptoid oligomers, pharmaceutical compositions and methods of using the same
AssigneeNew York University
InventorsKent Kirshenbaum, Mia L. Huang
Life of this patent
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Abstract
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.
Claims85
A peptoid oligomer according to formula I:
- or a pharmaceutically acceptable salt, solvate or prodrug thereof;
- and or a stereoisomer, isotopic variant or tautomer thereof;
- wherein
- each R1 is independently fluorenyl, 2-(indol-3-yl)ethyl, or a group selected from
- each R2 is independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, haloalkyl, halo, substituted or unsubstituted alkoxy, or cyano;
- each R3 is independently H, methyl, or phenyl;
- each R4 is independently H, or methyl;
- each R5 is independently —NR6aR6b;
- each R6a and R6b is independently H, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl;
- the subscript n is 0 or 1;
- the subscript m is 0, 1, 2, 3, or 4;
- the subscript t is 1, 2, 3, 4, or 5;
- the subscript u is 0, 1, or 2;
- the subscript v is 0, 1, 2, 3, 4, or 5;
- and * denotes the attachment point;
- and
- provided that
- i) at least one of R1s is
- and at least one of R1s is fluorenyl, 2-(indol-3-yl)ethyl, or a group selected from
- and
- ii) the compound is other than
- wherein R is —(CH2)3NH2
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Dependencies are inferred from the claim text.