Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates
[Display omitted] Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2015-06, Vol.25 (11), p.2314-2320 |
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| container_end_page | 2320 |
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| container_issue | 11 |
| container_start_page | 2314 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 25 |
| creator | Naumov, Roman N. Panda, Siva S. Girgis, Adel S. George, Riham F. Farhat, Michel Katritzky, Alan R. |
| description | [Display omitted]
Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties. |
| doi_str_mv | 10.1016/j.bmcl.2015.04.023 |
| format | Article |
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Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2015.04.023</identifier><identifier>PMID: 25937011</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Amino acids ; Animals ; Anti-inflammatory ; Anti-Inflammatory Agents - adverse effects ; Anti-Inflammatory Agents - chemistry ; Anti-Inflammatory Agents - pharmacology ; Conjugates ; Indomethacin - toxicity ; Mesalamine - adverse effects ; Mesalamine - chemistry ; Mesalamine - pharmacology ; Mesalazine ; Metronidazole ; Metronidazole - adverse effects ; Metronidazole - chemistry ; Metronidazole - pharmacology ; Mice ; Molecular Structure ; QSAR ; Quantitative Structure-Activity Relationship ; Stomach Ulcer - chemically induced</subject><ispartof>Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (11), p.2314-2320</ispartof><rights>2015 Elsevier Ltd</rights><rights>Copyright © 2015 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c426t-b373c8d7b0c8dd4b03c49fe28211c941a755b096a8de3360622e584e92aee28c3</citedby><cites>FETCH-LOGICAL-c426t-b373c8d7b0c8dd4b03c49fe28211c941a755b096a8de3360622e584e92aee28c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2015.04.023$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27926,27927,45997</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25937011$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Naumov, Roman N.</creatorcontrib><creatorcontrib>Panda, Siva S.</creatorcontrib><creatorcontrib>Girgis, Adel S.</creatorcontrib><creatorcontrib>George, Riham F.</creatorcontrib><creatorcontrib>Farhat, Michel</creatorcontrib><creatorcontrib>Katritzky, Alan R.</creatorcontrib><title>Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.</description><subject>Amino acids</subject><subject>Animals</subject><subject>Anti-inflammatory</subject><subject>Anti-Inflammatory Agents - adverse effects</subject><subject>Anti-Inflammatory Agents - chemistry</subject><subject>Anti-Inflammatory Agents - pharmacology</subject><subject>Conjugates</subject><subject>Indomethacin - toxicity</subject><subject>Mesalamine - adverse effects</subject><subject>Mesalamine - chemistry</subject><subject>Mesalamine - pharmacology</subject><subject>Mesalazine</subject><subject>Metronidazole</subject><subject>Metronidazole - adverse effects</subject><subject>Metronidazole - chemistry</subject><subject>Metronidazole - pharmacology</subject><subject>Mice</subject><subject>Molecular Structure</subject><subject>QSAR</subject><subject>Quantitative Structure-Activity Relationship</subject><subject>Stomach Ulcer - chemically induced</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM-O0zAQhy0Eot3CC3BAOXJJGP9JmkhcqhWwSJVWUJC4GceegKvELrZTqXviHXhDngRX3eXIZUYafb-fNB8hLyhUFGjzel_1kx4rBrSuQFTA-COypKIRJRdQPyZL6Boo2058XZCrGPcAVIAQT8mC1R1fA6VL8m13cukHRhsL5Uzxcbf5VMQ0m1Phh8L5I475nmxp3TCqaVLJh1OhdLJHLCaMalR31uGfX78nTME7a9SdH7HQ3u3n7yphfEaeDGqM-Px-r8iXd28_X9-U29v3H64321IL1qSy52uuW7PuIU8jeuBadAOyllGqO0HVuq77_I9qDXLeQMMY1q3AjinMlOYr8urSewj-54wxyclGjeOoHPo5Stq0OU4ZQEbZBdXBxxhwkIdgJxVOkoI8m5V7eTYrz2YlCJnN5tDL-_65n9D8izyozMCbC4D5y6PFIKO26DQaG1Anabz9X_9fj2mMMg</recordid><startdate>20150601</startdate><enddate>20150601</enddate><creator>Naumov, Roman N.</creator><creator>Panda, Siva S.</creator><creator>Girgis, Adel S.</creator><creator>George, Riham F.</creator><creator>Farhat, Michel</creator><creator>Katritzky, Alan R.</creator><general>Elsevier Ltd</general><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>20150601</creationdate><title>Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates</title><author>Naumov, Roman N. ; Panda, Siva S. ; Girgis, Adel S. ; George, Riham F. ; Farhat, Michel ; Katritzky, Alan R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c426t-b373c8d7b0c8dd4b03c49fe28211c941a755b096a8de3360622e584e92aee28c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Amino acids</topic><topic>Animals</topic><topic>Anti-inflammatory</topic><topic>Anti-Inflammatory Agents - adverse effects</topic><topic>Anti-Inflammatory Agents - chemistry</topic><topic>Anti-Inflammatory Agents - pharmacology</topic><topic>Conjugates</topic><topic>Indomethacin - toxicity</topic><topic>Mesalamine - adverse effects</topic><topic>Mesalamine - chemistry</topic><topic>Mesalamine - pharmacology</topic><topic>Mesalazine</topic><topic>Metronidazole</topic><topic>Metronidazole - adverse effects</topic><topic>Metronidazole - chemistry</topic><topic>Metronidazole - pharmacology</topic><topic>Mice</topic><topic>Molecular Structure</topic><topic>QSAR</topic><topic>Quantitative Structure-Activity Relationship</topic><topic>Stomach Ulcer - chemically induced</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Naumov, Roman N.</creatorcontrib><creatorcontrib>Panda, Siva S.</creatorcontrib><creatorcontrib>Girgis, Adel S.</creatorcontrib><creatorcontrib>George, Riham F.</creatorcontrib><creatorcontrib>Farhat, Michel</creatorcontrib><creatorcontrib>Katritzky, Alan R.</creatorcontrib><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>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Naumov, Roman N.</au><au>Panda, Siva S.</au><au>Girgis, Adel S.</au><au>George, Riham F.</au><au>Farhat, Michel</au><au>Katritzky, Alan R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2015-06-01</date><risdate>2015</risdate><volume>25</volume><issue>11</issue><spage>2314</spage><epage>2320</epage><pages>2314-2320</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>25937011</pmid><doi>10.1016/j.bmcl.2015.04.023</doi><tpages>7</tpages></addata></record> |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (11), p.2314-2320 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Amino acids Animals Anti-inflammatory Anti-Inflammatory Agents - adverse effects Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacology Conjugates Indomethacin - toxicity Mesalamine - adverse effects Mesalamine - chemistry Mesalamine - pharmacology Mesalazine Metronidazole Metronidazole - adverse effects Metronidazole - chemistry Metronidazole - pharmacology Mice Molecular Structure QSAR Quantitative Structure-Activity Relationship Stomach Ulcer - chemically induced |
| title | Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates |
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