Synthesis of Macromolecular Prodrugs of Procaine, Histamine and Isoniazid
The attachment of various drugs bearing-NH2 groups to poly-α, β-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical method. N-Ethyl-N'-(3-dimethylaminopropyl)c...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1989/08/25, Vol.37(8), pp.2245-2247 |
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| container_issue | 8 |
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| container_title | Chemical & pharmaceutical bulletin |
| container_volume | 37 |
| creator | GIAMMONA, Gaetano GIANNOLA, Libero Italo CARLISI, Bianca BAJARDI, Maria Luisa |
| description | The attachment of various drugs bearing-NH2 groups to poly-α, β-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical method. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) in an aqueous medium peoved to be useful in the attachment reaction. Isoniazid, procaine and histamine were covalently coupled as pendant groups onto poly-α, β-aspartic acid via an amide bond. In principle, controlled release of the aforementioned drugs can be achieved by biodegradation of the polymer or by cleavage of covalently bound polumer-drug conjugates. |
| doi_str_mv | 10.1248/cpb.37.2245 |
| format | Article |
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N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) in an aqueous medium peoved to be useful in the attachment reaction. Isoniazid, procaine and histamine were covalently coupled as pendant groups onto poly-α, β-aspartic acid via an amide bond. In principle, controlled release of the aforementioned drugs can be achieved by biodegradation of the polymer or by cleavage of covalently bound polumer-drug conjugates.</description><identifier>ISSN: 0009-2363</identifier><identifier>EISSN: 1347-5223</identifier><identifier>DOI: 10.1248/cpb.37.2245</identifier><identifier>PMID: 2598330</identifier><identifier>CODEN: CPBTAL</identifier><language>eng</language><publisher>Tokyo: The Pharmaceutical Society of Japan</publisher><subject><![CDATA[Biological and medical sciences ; Chemical Phenomena ; Chemistry ; General pharmacology ; histamine ; Histamine - administration & dosage ; Histamine - analogs & derivatives ; isoniazid ; Isoniazid - administration & dosage ; Isoniazid - analogs & derivatives ; macromolecular prodrug ; Medical sciences ; Molecular Weight ; pendant-chains system ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; poly-α, β-aspartic acid ; procaine ; Procaine - administration & dosage ; Procaine - analogs & derivatives ; Prodrugs - chemical synthesis]]></subject><ispartof>Chemical and Pharmaceutical Bulletin, 1989/08/25, Vol.37(8), pp.2245-2247</ispartof><rights>The Pharmaceutical Society of Japan</rights><rights>1990 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c607t-ecdcce5df49e06185acc0edf8d08326f58f4807411ae5daeec5d5a4d2c8531f33</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=6873124$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2598330$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>GIAMMONA, Gaetano</creatorcontrib><creatorcontrib>GIANNOLA, Libero Italo</creatorcontrib><creatorcontrib>CARLISI, Bianca</creatorcontrib><creatorcontrib>BAJARDI, Maria Luisa</creatorcontrib><title>Synthesis of Macromolecular Prodrugs of Procaine, Histamine and Isoniazid</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem. Pharm. Bull.</addtitle><description>The attachment of various drugs bearing-NH2 groups to poly-α, β-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical method. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) in an aqueous medium peoved to be useful in the attachment reaction. Isoniazid, procaine and histamine were covalently coupled as pendant groups onto poly-α, β-aspartic acid via an amide bond. In principle, controlled release of the aforementioned drugs can be achieved by biodegradation of the polymer or by cleavage of covalently bound polumer-drug conjugates.</description><subject>Biological and medical sciences</subject><subject>Chemical Phenomena</subject><subject>Chemistry</subject><subject>General pharmacology</subject><subject>histamine</subject><subject>Histamine - administration & dosage</subject><subject>Histamine - analogs & derivatives</subject><subject>isoniazid</subject><subject>Isoniazid - administration & dosage</subject><subject>Isoniazid - analogs & derivatives</subject><subject>macromolecular prodrug</subject><subject>Medical sciences</subject><subject>Molecular Weight</subject><subject>pendant-chains system</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>poly-α, β-aspartic acid</subject><subject>procaine</subject><subject>Procaine - administration & dosage</subject><subject>Procaine - analogs & derivatives</subject><subject>Prodrugs - chemical synthesis</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkM1P3DAQxa2qiC7QU8-Vcqh6oVn8ESfOsQJaVgJRCThbs_Z416t8bO3kAH99HTbaXmZGej-9p3mEfGF0yXihrsx-vRTVkvNCfiALJooql5yLj2RBKa1zLkrxiZzFuKOUS1qJU3LKZa2EoAuyenrthi1GH7PeZQ9gQt_2DZqxgZD9Cb0N4-ZdSrcB3-GP7M7HAdp0ZtDZbBX7zsObtxfkxEET8fO8z8nLr9vn67v8_vH36vrnfW5KWg05GmsMSuuKGmnJlARjKFqnLFWCl04qVyhaFYxBogDRSCuhsNwoKZgT4px8P_juQ_93xDjo1keDTQMd9mPUVS2SESsTeHkA008xBnR6H3wL4VUzqqfidCpOi0pPxSX662w7rlu0R3ZuKunfZh2igcYF6IyPR6xUlUieCbs5YLtU0gaPOoTBmwanSFZLNcXOY0r_L28haOzEP5mUjo0</recordid><startdate>1989</startdate><enddate>1989</enddate><creator>GIAMMONA, Gaetano</creator><creator>GIANNOLA, Libero Italo</creator><creator>CARLISI, Bianca</creator><creator>BAJARDI, Maria Luisa</creator><general>The Pharmaceutical Society of Japan</general><general>Maruzen</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>1989</creationdate><title>Synthesis of Macromolecular Prodrugs of Procaine, Histamine and Isoniazid</title><author>GIAMMONA, Gaetano ; GIANNOLA, Libero Italo ; CARLISI, Bianca ; BAJARDI, Maria Luisa</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c607t-ecdcce5df49e06185acc0edf8d08326f58f4807411ae5daeec5d5a4d2c8531f33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Biological and medical sciences</topic><topic>Chemical Phenomena</topic><topic>Chemistry</topic><topic>General pharmacology</topic><topic>histamine</topic><topic>Histamine - administration & dosage</topic><topic>Histamine - analogs & derivatives</topic><topic>isoniazid</topic><topic>Isoniazid - administration & dosage</topic><topic>Isoniazid - analogs & derivatives</topic><topic>macromolecular prodrug</topic><topic>Medical sciences</topic><topic>Molecular Weight</topic><topic>pendant-chains system</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>poly-α, β-aspartic acid</topic><topic>procaine</topic><topic>Procaine - administration & dosage</topic><topic>Procaine - analogs & derivatives</topic><topic>Prodrugs - chemical synthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>GIAMMONA, Gaetano</creatorcontrib><creatorcontrib>GIANNOLA, Libero Italo</creatorcontrib><creatorcontrib>CARLISI, Bianca</creatorcontrib><creatorcontrib>BAJARDI, Maria Luisa</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>GIAMMONA, Gaetano</au><au>GIANNOLA, Libero Italo</au><au>CARLISI, Bianca</au><au>BAJARDI, Maria Luisa</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of Macromolecular Prodrugs of Procaine, Histamine and Isoniazid</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>1989</date><risdate>1989</risdate><volume>37</volume><issue>8</issue><spage>2245</spage><epage>2247</epage><pages>2245-2247</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><coden>CPBTAL</coden><abstract>The attachment of various drugs bearing-NH2 groups to poly-α, β-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical method. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) in an aqueous medium peoved to be useful in the attachment reaction. Isoniazid, procaine and histamine were covalently coupled as pendant groups onto poly-α, β-aspartic acid via an amide bond. In principle, controlled release of the aforementioned drugs can be achieved by biodegradation of the polymer or by cleavage of covalently bound polumer-drug conjugates.</abstract><cop>Tokyo</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>2598330</pmid><doi>10.1248/cpb.37.2245</doi><tpages>3</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0009-2363 |
| ispartof | Chemical and Pharmaceutical Bulletin, 1989/08/25, Vol.37(8), pp.2245-2247 |
| issn | 0009-2363 1347-5223 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_79383216 |
| source | J-STAGE Free; MEDLINE; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Biological and medical sciences Chemical Phenomena Chemistry General pharmacology histamine Histamine - administration & dosage Histamine - analogs & derivatives isoniazid Isoniazid - administration & dosage Isoniazid - analogs & derivatives macromolecular prodrug Medical sciences Molecular Weight pendant-chains system Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments poly-α, β-aspartic acid procaine Procaine - administration & dosage Procaine - analogs & derivatives Prodrugs - chemical synthesis |
| title | Synthesis of Macromolecular Prodrugs of Procaine, Histamine and Isoniazid |
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