N,N-Dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents
The ability of some N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine–leucine–phenylalanine (f-...
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| Veröffentlicht in: | Farmaco (Società chimica italiana : 1989) 1999-07, Vol.54 (7), p.452-460 |
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| container_title | Farmaco (Società chimica italiana : 1989) |
| container_volume | 54 |
| creator | Mazzei, Mauro Sottofattori, Enzo Dondero, Ramona Ibrahim, Munjed Melloni, Edon Michetti, Mauro |
| description | The ability of some
N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine–leucine–phenylalanine (f-MLF) were used. The efficiency of the compounds was established by their capacity to reduce the O
2
− production by activated human neutrophils. Compounds carrying a 3-bis(2-methoxyethyl)amino group, a substituent found active in previously tested tricyclic compounds, do not show significant anti-PKC activity in this study. On the other hand, substitution with a 1-piperidinyl group leads all tested compounds to a high biological activity against stimulated neutrophils. |
| doi_str_mv | 10.1016/S0014-827X(99)00051-8 |
| format | Article |
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N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine–leucine–phenylalanine (f-MLF) were used. The efficiency of the compounds was established by their capacity to reduce the O
2
− production by activated human neutrophils. Compounds carrying a 3-bis(2-methoxyethyl)amino group, a substituent found active in previously tested tricyclic compounds, do not show significant anti-PKC activity in this study. On the other hand, substitution with a 1-piperidinyl group leads all tested compounds to a high biological activity against stimulated neutrophils.</description><identifier>ISSN: 0014-827X</identifier><identifier>EISSN: 1879-0569</identifier><identifier>DOI: 10.1016/S0014-827X(99)00051-8</identifier><identifier>PMID: 10486912</identifier><language>eng</language><publisher>Lausanne: Elsevier SAS</publisher><subject>1-Benzopyran-4-ones ; 5-Phenylisoxazoles ; Anti-inflammatory agents ; Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Anti-PKC activity ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Chromones - chemical synthesis ; Chromones - pharmacology ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - pharmacology ; Humans ; In Vitro Techniques ; Isoxazoles - chemical synthesis ; Isoxazoles - pharmacology ; Medical sciences ; Neutrophil Activation - drug effects ; Neutrophils ; Neutrophils - drug effects ; Neutrophils - metabolism ; Pharmacology. Drug treatments ; Protein Kinase C - antagonists & inhibitors ; Superoxide anion ; Superoxides - metabolism</subject><ispartof>Farmaco (Società chimica italiana : 1989), 1999-07, Vol.54 (7), p.452-460</ispartof><rights>1999 Elsevier Science S.A.</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c456t-5717f3c1837ee7a13e2439ee7cc8b24666734133003ec4a1dd3b5467823f028e3</citedby><cites>FETCH-LOGICAL-c456t-5717f3c1837ee7a13e2439ee7cc8b24666734133003ec4a1dd3b5467823f028e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1937057$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10486912$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mazzei, Mauro</creatorcontrib><creatorcontrib>Sottofattori, Enzo</creatorcontrib><creatorcontrib>Dondero, Ramona</creatorcontrib><creatorcontrib>Ibrahim, Munjed</creatorcontrib><creatorcontrib>Melloni, Edon</creatorcontrib><creatorcontrib>Michetti, Mauro</creatorcontrib><title>N,N-Dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents</title><title>Farmaco (Società chimica italiana : 1989)</title><addtitle>Farmaco</addtitle><description>The ability of some
N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine–leucine–phenylalanine (f-MLF) were used. The efficiency of the compounds was established by their capacity to reduce the O
2
− production by activated human neutrophils. Compounds carrying a 3-bis(2-methoxyethyl)amino group, a substituent found active in previously tested tricyclic compounds, do not show significant anti-PKC activity in this study. On the other hand, substitution with a 1-piperidinyl group leads all tested compounds to a high biological activity against stimulated neutrophils.</description><subject>1-Benzopyran-4-ones</subject><subject>5-Phenylisoxazoles</subject><subject>Anti-inflammatory agents</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</subject><subject>Anti-PKC activity</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Chromones - chemical synthesis</subject><subject>Chromones - pharmacology</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Isoxazoles - chemical synthesis</subject><subject>Isoxazoles - pharmacology</subject><subject>Medical sciences</subject><subject>Neutrophil Activation - drug effects</subject><subject>Neutrophils</subject><subject>Neutrophils - drug effects</subject><subject>Neutrophils - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Kinase C - antagonists & inhibitors</subject><subject>Superoxide anion</subject><subject>Superoxides - metabolism</subject><issn>0014-827X</issn><issn>1879-0569</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1v1DAQhi0EosvSnwDKASGQCNix449ThVq-pKocSqWqF8vrTMCQxFuPg7r8-nq7K-DWk2c0z-sZPYQ8Y_Qto0y-O6eUiVo36vKVMa8ppS2r9QOyYFqZmrbSPCSLv8gBeYL4s7RKSfWYHDAqtDSsWZCrszdn9Ulww6_N4MYwRZxXmEOeM3SV_5HiGCfAyk1dFTDeuD9x2LZYrWOGKZdgmeVQh6kv-dHlmDaV-15G-JQ86t2AcLh_l-Ti44dvx5_r06-fvhy_P629aGWuW8VUzz3TXAEoxzg0gptSeq9XjZBSKi4Y55Ry8MKxruOrVkilG97TRgNfkpe7f9cpXs-A2Y4BPQyDmyDOaBWlotEFX5J2B_oUERP0dp3C6NLGMmq3Uu2dVLs1Zo2xd1KtLrnn-wXzaoTuv9TOYgFe7AGH3g19cpMP-I8zXNFWFexoh0Gx8TtAsugDTB66kMBn28VwzyW36FeUdg</recordid><startdate>19990730</startdate><enddate>19990730</enddate><creator>Mazzei, Mauro</creator><creator>Sottofattori, Enzo</creator><creator>Dondero, Ramona</creator><creator>Ibrahim, Munjed</creator><creator>Melloni, Edon</creator><creator>Michetti, Mauro</creator><general>Elsevier SAS</general><general>Elsevier Science</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>19990730</creationdate><title>N,N-Dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents</title><author>Mazzei, Mauro ; Sottofattori, Enzo ; Dondero, Ramona ; Ibrahim, Munjed ; Melloni, Edon ; Michetti, Mauro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c456t-5717f3c1837ee7a13e2439ee7cc8b24666734133003ec4a1dd3b5467823f028e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>1-Benzopyran-4-ones</topic><topic>5-Phenylisoxazoles</topic><topic>Anti-inflammatory agents</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</topic><topic>Anti-PKC activity</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Chromones - chemical synthesis</topic><topic>Chromones - pharmacology</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Isoxazoles - chemical synthesis</topic><topic>Isoxazoles - pharmacology</topic><topic>Medical sciences</topic><topic>Neutrophil Activation - drug effects</topic><topic>Neutrophils</topic><topic>Neutrophils - drug effects</topic><topic>Neutrophils - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Kinase C - antagonists & inhibitors</topic><topic>Superoxide anion</topic><topic>Superoxides - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mazzei, Mauro</creatorcontrib><creatorcontrib>Sottofattori, Enzo</creatorcontrib><creatorcontrib>Dondero, Ramona</creatorcontrib><creatorcontrib>Ibrahim, Munjed</creatorcontrib><creatorcontrib>Melloni, Edon</creatorcontrib><creatorcontrib>Michetti, Mauro</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>Farmaco (Società chimica italiana : 1989)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mazzei, Mauro</au><au>Sottofattori, Enzo</au><au>Dondero, Ramona</au><au>Ibrahim, Munjed</au><au>Melloni, Edon</au><au>Michetti, Mauro</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>N,N-Dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents</atitle><jtitle>Farmaco (Società chimica italiana : 1989)</jtitle><addtitle>Farmaco</addtitle><date>1999-07-30</date><risdate>1999</risdate><volume>54</volume><issue>7</issue><spage>452</spage><epage>460</epage><pages>452-460</pages><issn>0014-827X</issn><eissn>1879-0569</eissn><abstract>The ability of some
N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine–leucine–phenylalanine (f-MLF) were used. The efficiency of the compounds was established by their capacity to reduce the O
2
− production by activated human neutrophils. Compounds carrying a 3-bis(2-methoxyethyl)amino group, a substituent found active in previously tested tricyclic compounds, do not show significant anti-PKC activity in this study. On the other hand, substitution with a 1-piperidinyl group leads all tested compounds to a high biological activity against stimulated neutrophils.</abstract><cop>Lausanne</cop><pub>Elsevier SAS</pub><pmid>10486912</pmid><doi>10.1016/S0014-827X(99)00051-8</doi><tpages>9</tpages></addata></record> |
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| subjects | 1-Benzopyran-4-ones 5-Phenylisoxazoles Anti-inflammatory agents Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - pharmacology Anti-PKC activity Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Chromones - chemical synthesis Chromones - pharmacology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Humans In Vitro Techniques Isoxazoles - chemical synthesis Isoxazoles - pharmacology Medical sciences Neutrophil Activation - drug effects Neutrophils Neutrophils - drug effects Neutrophils - metabolism Pharmacology. Drug treatments Protein Kinase C - antagonists & inhibitors Superoxide anion Superoxides - metabolism |
| title | N,N-Dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents |
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