SYNTHESIS OF CONJUGATES OF OLIGOPEPTIDES AND ANTIMETABOLITES.
Item
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Title
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SYNTHESIS OF CONJUGATES OF OLIGOPEPTIDES AND ANTIMETABOLITES.
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Identifier
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AAI8319797
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identifier
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8319797
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Creator
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SHEIKH, MAQSOOD A.
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Contributor
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Robert Engel
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Date
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1983
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Language
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English
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Publisher
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City University of New York.
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Subject
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Chemistry, Biochemistry
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Abstract
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The present thesis program has had as its purpose the synthesis of phosphonic acid analogues of natural phosphates bound to oligopeptides. The purpose of oligopeptide is to enable transport of potential agents that might serve as drugs for metabolic regulation via the oligopeptide transport system. This was to be accomplished by the attachement of the isosteric phosphonic acid analogue, i.e., 3,4-dihydroxybutyl-1-phosphonic acid (DHBP) and 4-hydroxy-3-oxobutyl-1-phosphonic acid (DHAP(,a)) to the (beta)-carboxyl group of the aspartyl unit in the tripeptide aspartylalanylalanine and alanylaspartylalanine. In addition, the conjugation of the isosteric phosphonic acid analogue of phosphomevalonate, 5-carboxy-4-hydroxy-4-methylpentyl-1-phosphonic acid and nalidixic acid with alanylserylalanine and the conjugation of sulfanilamide and other drugs to aspartylalanylalanine were performed.;The studies on peptide transport in barley have shown that peptides may be of considerable importance in certain plant systems and considering these studies, we have tried to use aspartylalanylalanine in the transport of certain antimetabolites into fruit plants.;Initially, the potential for in vivo antimetabolic activity for dihydroxyacetone phosphate was not promising due to the lack of transport mechanism for the natural material. However, in vivo activity has been accomplished by the coupling of 3,4-dihydroxybutyl-1-phosphonic acid and 4-hydroxy-3-oxobutyl-1-phosphonic acid with the aspartylalanylalanine.
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Type
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dissertation
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Source
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PQT Legacy CUNY.xlsx
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degree
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Ph.D.
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Program
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Chemistry
