Phenylboronic acid complexes derived from aminosalicylic acid for bioconjugate preparation

摘要

The present invention relates to a novel class of bioconjugates derived from phenylboronic acid complexes, and the method of making and using such bioconjugate complexes. The complexes are in the form of the following general formulas. ##STR1## wherein group Q is selected from either O, S, NH, N-alkyl and N-aryl, wherein alkyl denotes a hydrocarbon moiety, wherein aryl is selected from either an aromatic ring, a substituted aromatic ring and fused aromatic rings, wherein group R is preferably selected from either O, NH, CH.sub.2, alkyl and aryl, wherein alkyl and aryl are as were previously defined,PP wherein group X is selected from either H, CH.sub.3 and C.sub.6 H.sub.5, wherein group Y is selected from either O, NH, CH.sub.2, alkyl and aryl, wherein alkyl and aryl are as were previously defined,PP wherein groups Z and Z* comprises spacers selected from either alkyl and polyethyleneglycol chains, of from 1 to 16 carbon equivalents in length, wherein the chain may contain intermediate amide and disulfide bonds, and wherein groups Z and Z* are preferably selected from, but not limited to, either (CH.sub.2).sub.n, wherein n=1 to 5, and (CH.sub.2 CH.sub.2 O).sub. n', wherein n'=2 to 4,PPand wherein groups BAS and BAS* are bioactive species.