On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase
The relative inhibitory potency of imidazole and derivatives on thromboxane synthetase from human platelets was found to be increased by substitution of the 1-position and abolished in other positions. The potency of 1-substituted imidazoles was increased as the side chain became more hydrophobic. A...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1978-01, Vol.80 (1), p.236-242 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Tai, Hsin-Hsiung Yuan, Barbara |
| description | The relative inhibitory potency of imidazole and derivatives on thromboxane synthetase from human platelets was found to be increased by substitution of the 1-position and abolished in other positions. The potency of 1-substituted imidazoles was increased as the side chain became more hydrophobic. Among the imidazole derivatives tested 1-nonyl-imidazole and 1-(2-isopropyl phenyl)-imidazole showed the highest potency with I
50 in the range of 10
−8 M. Inhibition by imidazole and its derivatives appeared to be very specific for thromboxane synthetase since other enzymes in prostaglandin endoperoxide metabolism were not affected. Kinetic studies indicated that inhibition was competitive with respect to prostaglandin endoperoxide substrate. |
| doi_str_mv | 10.1016/0006-291X(78)91128-2 |
| format | Article |
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50 in the range of 10
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50 in the range of 10
−8 M. Inhibition by imidazole and its derivatives appeared to be very specific for thromboxane synthetase since other enzymes in prostaglandin endoperoxide metabolism were not affected. Kinetic studies indicated that inhibition was competitive with respect to prostaglandin endoperoxide substrate.</description><subject>Animals</subject><subject>Blood Platelets - enzymology</subject><subject>Imidazoles - pharmacology</subject><subject>Kinetics</subject><subject>Lung - enzymology</subject><subject>Microsomes - enzymology</subject><subject>Oxidoreductases - antagonists & inhibitors</subject><subject>Prostaglandins - biosynthesis</subject><subject>Radioimmunoassay</subject><subject>Sheep</subject><subject>Structure-Activity Relationship</subject><subject>Thromboxane-A Synthase - antagonists & inhibitors</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1978</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LxDAQhoP4tX78Aw85iR6qmaZN0osgi18geFHwFtJkipFtsybZxfXX23XFo6c5zPs-zDyEnAC7AAbikjEmirKB1zOpzhuAUhXlFpkAa1hRAqu2yeQvsk8OUnpnDKASzR7ZFSUXdTUhz08DzW9I_fDmW59DXNF5yDjYFQ0d9b135ivMkJrBUZ8TdRj90mS_xETDuhpD34ZPMyBNq2EkZZPwiOx0Zpbw-Hcekpfbm-fpffH4dPcwvX4sLK9FLqATykqURirrTA01OqU4U04Ab5w0NZcltKrCjiEKZyzHSjWyYs62zAHwQ3K64c5j-Fhgyrr3yeJsNp4TFkkrrjgHqcZgtQnaGFKK2Ol59L2JKw1Mr13qtSi9FqWl0j8udTnWTn75i7ZH91fayBvXV5s1jj8uPUadrB_VofMRbdYu-P_53yOphIY</recordid><startdate>19780113</startdate><enddate>19780113</enddate><creator>Tai, Hsin-Hsiung</creator><creator>Yuan, Barbara</creator><general>Elsevier Inc</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>19780113</creationdate><title>On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase</title><author>Tai, Hsin-Hsiung ; Yuan, Barbara</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-1f68c7e7a78cda515ed88308d6139d7a53721b84ef0ee6dac3e489740dcb0d113</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1978</creationdate><topic>Animals</topic><topic>Blood Platelets - enzymology</topic><topic>Imidazoles - pharmacology</topic><topic>Kinetics</topic><topic>Lung - enzymology</topic><topic>Microsomes - enzymology</topic><topic>Oxidoreductases - antagonists & inhibitors</topic><topic>Prostaglandins - biosynthesis</topic><topic>Radioimmunoassay</topic><topic>Sheep</topic><topic>Structure-Activity Relationship</topic><topic>Thromboxane-A Synthase - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tai, Hsin-Hsiung</creatorcontrib><creatorcontrib>Yuan, Barbara</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>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tai, Hsin-Hsiung</au><au>Yuan, Barbara</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1978-01-13</date><risdate>1978</risdate><volume>80</volume><issue>1</issue><spage>236</spage><epage>242</epage><pages>236-242</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>The relative inhibitory potency of imidazole and derivatives on thromboxane synthetase from human platelets was found to be increased by substitution of the 1-position and abolished in other positions. The potency of 1-substituted imidazoles was increased as the side chain became more hydrophobic. Among the imidazole derivatives tested 1-nonyl-imidazole and 1-(2-isopropyl phenyl)-imidazole showed the highest potency with I
50 in the range of 10
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| ispartof | Biochemical and biophysical research communications, 1978-01, Vol.80 (1), p.236-242 |
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| language | eng |
| recordid | cdi_proquest_miscellaneous_83833178 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Blood Platelets - enzymology Imidazoles - pharmacology Kinetics Lung - enzymology Microsomes - enzymology Oxidoreductases - antagonists & inhibitors Prostaglandins - biosynthesis Radioimmunoassay Sheep Structure-Activity Relationship Thromboxane-A Synthase - antagonists & inhibitors |
| title | On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase |
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