Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes
A series of new substituted pyrazoles embedded with a variety of function groups has been synthesized from 4-[4-(1,2-dihydro-2,3-dimethyl-1-phenyl-5-oxo-3H-pyrazol-4-yl)]-2-cyano-4-oxo-butanenitrile ( 4 ). The synthesized compounds were fully characterized and their structures were elucidated based...
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| Veröffentlicht in: | Journal of the Iranian Chemical Society 2018-08, Vol.15 (8), p.1785-1800 |
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| container_title | Journal of the Iranian Chemical Society |
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| creator | Eldebss, Taha M. A. Yi, Xue-Jing Farag, Ahmad M. Khedr, Ahmad A. Abdulla, Mohamed M. Mabkhot, Yahia N. |
| description | A series of new substituted pyrazoles embedded with a variety of function groups has been synthesized from 4-[4-(1,2-dihydro-2,3-dimethyl-1-phenyl-5-oxo-3H-pyrazol-4-yl)]-2-cyano-4-oxo-butanenitrile (
4
). The synthesized compounds were fully characterized and their structures were elucidated based on elemental analysis, spectral data, and alternative synthetic pathways, whenever possible. The pharmacological activities of these new compounds as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes have been investigated and compared to the most common inhibitors of MAO enzymes used to treat depression and anxiety such as deprenyl (selegiline), moclobemide, and clorgyline drugs. The most potent of the synthesized compounds was
4, 11
, and
53
which showed higher inhibition activity toward type A MAO enzyme and even exceeded that of deprenyl, moclobemide, and clorgyline drugs. |
| doi_str_mv | 10.1007/s13738-018-1376-1 |
| format | Article |
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4
). The synthesized compounds were fully characterized and their structures were elucidated based on elemental analysis, spectral data, and alternative synthetic pathways, whenever possible. The pharmacological activities of these new compounds as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes have been investigated and compared to the most common inhibitors of MAO enzymes used to treat depression and anxiety such as deprenyl (selegiline), moclobemide, and clorgyline drugs. The most potent of the synthesized compounds was
4, 11
, and
53
which showed higher inhibition activity toward type A MAO enzyme and even exceeded that of deprenyl, moclobemide, and clorgyline drugs.</description><identifier>ISSN: 1735-207X</identifier><identifier>EISSN: 1735-2428</identifier><identifier>DOI: 10.1007/s13738-018-1376-1</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Analytical Chemistry ; Anxiety ; Biochemistry ; Chemical synthesis ; Chemistry ; Chemistry and Materials Science ; Enzymes ; Inhibitors ; Inorganic Chemistry ; Mental depression ; Organic Chemistry ; Original Paper ; Oxidase ; Pharmacology ; Physical Chemistry ; Pyrazolones</subject><ispartof>Journal of the Iranian Chemical Society, 2018-08, Vol.15 (8), p.1785-1800</ispartof><rights>Iranian Chemical Society 2018</rights><rights>Copyright Springer Science & Business Media 2018</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c316t-c8afccb6e5994f86fdd7cf5809dbf6b81f8c608577003a6b095159fb2a8d27983</citedby><cites>FETCH-LOGICAL-c316t-c8afccb6e5994f86fdd7cf5809dbf6b81f8c608577003a6b095159fb2a8d27983</cites><orcidid>0000-0002-1922-5037</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s13738-018-1376-1$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s13738-018-1376-1$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids></links><search><creatorcontrib>Eldebss, Taha M. A.</creatorcontrib><creatorcontrib>Yi, Xue-Jing</creatorcontrib><creatorcontrib>Farag, Ahmad M.</creatorcontrib><creatorcontrib>Khedr, Ahmad A.</creatorcontrib><creatorcontrib>Abdulla, Mohamed M.</creatorcontrib><creatorcontrib>Mabkhot, Yahia N.</creatorcontrib><title>Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes</title><title>Journal of the Iranian Chemical Society</title><addtitle>J IRAN CHEM SOC</addtitle><description>A series of new substituted pyrazoles embedded with a variety of function groups has been synthesized from 4-[4-(1,2-dihydro-2,3-dimethyl-1-phenyl-5-oxo-3H-pyrazol-4-yl)]-2-cyano-4-oxo-butanenitrile (
4
). The synthesized compounds were fully characterized and their structures were elucidated based on elemental analysis, spectral data, and alternative synthetic pathways, whenever possible. The pharmacological activities of these new compounds as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes have been investigated and compared to the most common inhibitors of MAO enzymes used to treat depression and anxiety such as deprenyl (selegiline), moclobemide, and clorgyline drugs. The most potent of the synthesized compounds was
4, 11
, and
53
which showed higher inhibition activity toward type A MAO enzyme and even exceeded that of deprenyl, moclobemide, and clorgyline drugs.</description><subject>Analytical Chemistry</subject><subject>Anxiety</subject><subject>Biochemistry</subject><subject>Chemical synthesis</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Enzymes</subject><subject>Inhibitors</subject><subject>Inorganic Chemistry</subject><subject>Mental depression</subject><subject>Organic Chemistry</subject><subject>Original Paper</subject><subject>Oxidase</subject><subject>Pharmacology</subject><subject>Physical Chemistry</subject><subject>Pyrazolones</subject><issn>1735-207X</issn><issn>1735-2428</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><recordid>eNp1kM1KAzEURoMoWKsP4C7gOppMJn9LKWqFggsVdBUymcRO6SQ1maLTp3fqKK7c3HsX3_kuHADOCb4kGIurTKigEmEi0XBxRA7AhAjKUFEW8vD3xuLlGJzkvMKYCczKCXh97EO3dLnJMHoY3Afc9Mns4joGhyqTXQ2XrnMp2t6uXYYmwyYsm6rpYvpG2hiiaZvgYPxs6gGALuz61uVTcOTNOruznz0Fz7c3T7M5Wjzc3c-uF8hSwjtkpfHWVtwxpUovua9rYT2TWNWV55UkXlqOJRMCY2p4hRUjTPmqMLIuhJJ0Ci7G3k2K71uXO72K2xSGl7rAnFKiilINKTKmbIo5J-f1JjWtSb0mWO8N6tGgHgzqvcFhTEExMnnIhjeX_pr_h74AZ691PA</recordid><startdate>20180801</startdate><enddate>20180801</enddate><creator>Eldebss, Taha M. A.</creator><creator>Yi, Xue-Jing</creator><creator>Farag, Ahmad M.</creator><creator>Khedr, Ahmad A.</creator><creator>Abdulla, Mohamed M.</creator><creator>Mabkhot, Yahia N.</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0002-1922-5037</orcidid></search><sort><creationdate>20180801</creationdate><title>Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes</title><author>Eldebss, Taha M. A. ; Yi, Xue-Jing ; Farag, Ahmad M. ; Khedr, Ahmad A. ; Abdulla, Mohamed M. ; Mabkhot, Yahia N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c316t-c8afccb6e5994f86fdd7cf5809dbf6b81f8c608577003a6b095159fb2a8d27983</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Analytical Chemistry</topic><topic>Anxiety</topic><topic>Biochemistry</topic><topic>Chemical synthesis</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Enzymes</topic><topic>Inhibitors</topic><topic>Inorganic Chemistry</topic><topic>Mental depression</topic><topic>Organic Chemistry</topic><topic>Original Paper</topic><topic>Oxidase</topic><topic>Pharmacology</topic><topic>Physical Chemistry</topic><topic>Pyrazolones</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Eldebss, Taha M. A.</creatorcontrib><creatorcontrib>Yi, Xue-Jing</creatorcontrib><creatorcontrib>Farag, Ahmad M.</creatorcontrib><creatorcontrib>Khedr, Ahmad A.</creatorcontrib><creatorcontrib>Abdulla, Mohamed M.</creatorcontrib><creatorcontrib>Mabkhot, Yahia N.</creatorcontrib><collection>CrossRef</collection><jtitle>Journal of the Iranian Chemical Society</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Eldebss, Taha M. A.</au><au>Yi, Xue-Jing</au><au>Farag, Ahmad M.</au><au>Khedr, Ahmad A.</au><au>Abdulla, Mohamed M.</au><au>Mabkhot, Yahia N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes</atitle><jtitle>Journal of the Iranian Chemical Society</jtitle><stitle>J IRAN CHEM SOC</stitle><date>2018-08-01</date><risdate>2018</risdate><volume>15</volume><issue>8</issue><spage>1785</spage><epage>1800</epage><pages>1785-1800</pages><issn>1735-207X</issn><eissn>1735-2428</eissn><abstract>A series of new substituted pyrazoles embedded with a variety of function groups has been synthesized from 4-[4-(1,2-dihydro-2,3-dimethyl-1-phenyl-5-oxo-3H-pyrazol-4-yl)]-2-cyano-4-oxo-butanenitrile (
4
). The synthesized compounds were fully characterized and their structures were elucidated based on elemental analysis, spectral data, and alternative synthetic pathways, whenever possible. The pharmacological activities of these new compounds as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes have been investigated and compared to the most common inhibitors of MAO enzymes used to treat depression and anxiety such as deprenyl (selegiline), moclobemide, and clorgyline drugs. The most potent of the synthesized compounds was
4, 11
, and
53
which showed higher inhibition activity toward type A MAO enzyme and even exceeded that of deprenyl, moclobemide, and clorgyline drugs.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><doi>10.1007/s13738-018-1376-1</doi><tpages>16</tpages><orcidid>https://orcid.org/0000-0002-1922-5037</orcidid></addata></record> |
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| subjects | Analytical Chemistry Anxiety Biochemistry Chemical synthesis Chemistry Chemistry and Materials Science Enzymes Inhibitors Inorganic Chemistry Mental depression Organic Chemistry Original Paper Oxidase Pharmacology Physical Chemistry Pyrazolones |
| title | Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes |
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