Antifertility potential of ornidazole analogues in rats
In order to determine which part of the ornidazole molecule [1‐(3‐chloro‐2‐hydroxy)propyhl‐2‐methyl‐5‐nitroimidazole] is responsible for its antifertility action, structural analogues were fed to male rats of proven fertility at doses equivalent to the antifertility dose of ornidazole (1.82 mmol/kg/...
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Veröffentlicht in: | Journal of andrology 1997-07, Vol.18 (4), p.431-438 |
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description | In order to determine which part of the ornidazole molecule [1‐(3‐chloro‐2‐hydroxy)propyhl‐2‐methyl‐5‐nitroimidazole] is responsible for its antifertility action, structural analogues were fed to male rats of proven fertility at doses equivalent to the antifertility dose of ornidazole (1.82 mmol/kg/day). The fertility of the males was tested, before oral gavage (control mating) and after 10 and 14 days of feeding, by counting the number of fetuses and corpora lutea present in females 12 days after mating. The day after the last mating, the kinematic parameters of sperm from the cauda epididymldis were assessed objectively with a Hamilton‐Thome motility analyzer. Analogues bearing the 2‐nitro and 5‐methyl groups on the imidazole ring were inactive if the (chlorohydroxy)propyl group were substituted by proton or methyl, hydroxyethyl, chloroethyl, or (sulfonylethyl)ethyl groups, indicating that the three‐carbon side chain of ornidazole was necessary for the antifertility action. Only ornidazole and its acetate were effective antifertility agents, but a compound bearing the (chlorohydroxy)propyi side chain attached to a nitrogen atom of a heterocyclic phthalimide produced a partial but temporary reduction in fertility. Similarities of the action of ornidazole with the male antifertility agent, α‐chbrohydrin [3‐chloro‐1,2‐propanediol], are discussed. |
doi_str_mv | 10.1002/j.1939-4640.1997.tb01949.x |
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G ; Yeung, C. H ; Skupin, R ; Haufe, G</creator><creatorcontrib>Cooper, T. G ; Yeung, C. H ; Skupin, R ; Haufe, G</creatorcontrib><description>In order to determine which part of the ornidazole molecule [1‐(3‐chloro‐2‐hydroxy)propyhl‐2‐methyl‐5‐nitroimidazole] is responsible for its antifertility action, structural analogues were fed to male rats of proven fertility at doses equivalent to the antifertility dose of ornidazole (1.82 mmol/kg/day). The fertility of the males was tested, before oral gavage (control mating) and after 10 and 14 days of feeding, by counting the number of fetuses and corpora lutea present in females 12 days after mating. The day after the last mating, the kinematic parameters of sperm from the cauda epididymldis were assessed objectively with a Hamilton‐Thome motility analyzer. Analogues bearing the 2‐nitro and 5‐methyl groups on the imidazole ring were inactive if the (chlorohydroxy)propyl group were substituted by proton or methyl, hydroxyethyl, chloroethyl, or (sulfonylethyl)ethyl groups, indicating that the three‐carbon side chain of ornidazole was necessary for the antifertility action. Only ornidazole and its acetate were effective antifertility agents, but a compound bearing the (chlorohydroxy)propyi side chain attached to a nitrogen atom of a heterocyclic phthalimide produced a partial but temporary reduction in fertility. Similarities of the action of ornidazole with the male antifertility agent, α‐chbrohydrin [3‐chloro‐1,2‐propanediol], are discussed.</description><identifier>ISSN: 0196-3635</identifier><identifier>EISSN: 1939-4640</identifier><identifier>DOI: 10.1002/j.1939-4640.1997.tb01949.x</identifier><identifier>PMID: 9283957</identifier><identifier>CODEN: JOAND3</identifier><language>eng</language><publisher>Oxford, UK: Am Soc Andrology</publisher><subject>Animals ; Biological and medical sciences ; Birth control ; Body Weight - drug effects ; CASA ; contraception ; Contraceptive Agents, Male - pharmacology ; Epididymis ; fertility ; Fertility - drug effects ; Gynecology. Andrology. Obstetrics ; Hematocrit ; Male ; Medical sciences ; nitroimidazoles ; Organ Size - drug effects ; Ornidazole - analogs & derivatives ; Ornidazole - pharmacology ; Other methods of contraception. Sterilization ; Rats ; Rats, Sprague-Dawley ; sperm motility ; Sperm Motility - drug effects</subject><ispartof>Journal of andrology, 1997-07, Vol.18 (4), p.431-438</ispartof><rights>1997 American Society of Andrology</rights><rights>1997 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4829-4c9e4560b46626adc71420cb684ac0847581f2e7d0350ddaaa4317bf722c60fe3</citedby><cites>FETCH-LOGICAL-c4829-4c9e4560b46626adc71420cb684ac0847581f2e7d0350ddaaa4317bf722c60fe3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fj.1939-4640.1997.tb01949.x$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fj.1939-4640.1997.tb01949.x$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1433,27924,27925,46409,46833</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2816371$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9283957$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cooper, T. G</creatorcontrib><creatorcontrib>Yeung, C. H</creatorcontrib><creatorcontrib>Skupin, R</creatorcontrib><creatorcontrib>Haufe, G</creatorcontrib><title>Antifertility potential of ornidazole analogues in rats</title><title>Journal of andrology</title><addtitle>J Androl</addtitle><description>In order to determine which part of the ornidazole molecule [1‐(3‐chloro‐2‐hydroxy)propyhl‐2‐methyl‐5‐nitroimidazole] is responsible for its antifertility action, structural analogues were fed to male rats of proven fertility at doses equivalent to the antifertility dose of ornidazole (1.82 mmol/kg/day). The fertility of the males was tested, before oral gavage (control mating) and after 10 and 14 days of feeding, by counting the number of fetuses and corpora lutea present in females 12 days after mating. The day after the last mating, the kinematic parameters of sperm from the cauda epididymldis were assessed objectively with a Hamilton‐Thome motility analyzer. Analogues bearing the 2‐nitro and 5‐methyl groups on the imidazole ring were inactive if the (chlorohydroxy)propyl group were substituted by proton or methyl, hydroxyethyl, chloroethyl, or (sulfonylethyl)ethyl groups, indicating that the three‐carbon side chain of ornidazole was necessary for the antifertility action. Only ornidazole and its acetate were effective antifertility agents, but a compound bearing the (chlorohydroxy)propyi side chain attached to a nitrogen atom of a heterocyclic phthalimide produced a partial but temporary reduction in fertility. Similarities of the action of ornidazole with the male antifertility agent, α‐chbrohydrin [3‐chloro‐1,2‐propanediol], are discussed.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Birth control</subject><subject>Body Weight - drug effects</subject><subject>CASA</subject><subject>contraception</subject><subject>Contraceptive Agents, Male - pharmacology</subject><subject>Epididymis</subject><subject>fertility</subject><subject>Fertility - drug effects</subject><subject>Gynecology. Andrology. Obstetrics</subject><subject>Hematocrit</subject><subject>Male</subject><subject>Medical sciences</subject><subject>nitroimidazoles</subject><subject>Organ Size - drug effects</subject><subject>Ornidazole - analogs & derivatives</subject><subject>Ornidazole - pharmacology</subject><subject>Other methods of contraception. Sterilization</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>sperm motility</subject><subject>Sperm Motility - drug effects</subject><issn>0196-3635</issn><issn>1939-4640</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkM1u2zAQhImiReo4eYQCQtHmJod_IsWeajhp0yBoLsmZWFFUQoOWXFKG7D59KFjwPScSuzOzux9CXwleEIzp9XpBFFM5FzwVlJKLvsJEcbXYf0CzU-sjmqWqyJlgxWd0HuM6eTGR7AydKVoyVcgZksu2d40NvfOuP2TbrrepAD7rmqwLravhf-dtBi347mVnY-baLEAfL9CnBny0l9M7R8-_bp9Wd_nD4-8_q-VDbnhJ0x5GWV4IXHEhqIDaSMIpNpUoORhcclmUpKFW1pgVuK4BgDMiq0ZSagRuLJujq2PuNnT_0vxeb1w01ntobbeLWipaFCqdOEc_jkITuhiDbfQ2uA2EgyZYj9T0Wo9o9IhGj9T0RE3vk_nLNGVXbWx9sk6YUv_b1IdowDcBWuPiSUZLIpgkSfbzKBuct4d3LKDvl39vxm-K-H6MeHUvr4MLVscNeJ_2InoYBlJqrhMi9gZS1JaP</recordid><startdate>199707</startdate><enddate>199707</enddate><creator>Cooper, T. G</creator><creator>Yeung, C. H</creator><creator>Skupin, R</creator><creator>Haufe, G</creator><general>Am Soc Andrology</general><general>Blackwell Publishing Ltd</general><general>American Society of Andrology</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>199707</creationdate><title>Antifertility potential of ornidazole analogues in rats</title><author>Cooper, T. G ; Yeung, C. H ; Skupin, R ; Haufe, G</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4829-4c9e4560b46626adc71420cb684ac0847581f2e7d0350ddaaa4317bf722c60fe3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Birth control</topic><topic>Body Weight - drug effects</topic><topic>CASA</topic><topic>contraception</topic><topic>Contraceptive Agents, Male - pharmacology</topic><topic>Epididymis</topic><topic>fertility</topic><topic>Fertility - drug effects</topic><topic>Gynecology. Andrology. Obstetrics</topic><topic>Hematocrit</topic><topic>Male</topic><topic>Medical sciences</topic><topic>nitroimidazoles</topic><topic>Organ Size - drug effects</topic><topic>Ornidazole - analogs & derivatives</topic><topic>Ornidazole - pharmacology</topic><topic>Other methods of contraception. Sterilization</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>sperm motility</topic><topic>Sperm Motility - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cooper, T. G</creatorcontrib><creatorcontrib>Yeung, C. H</creatorcontrib><creatorcontrib>Skupin, R</creatorcontrib><creatorcontrib>Haufe, G</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>Journal of andrology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cooper, T. G</au><au>Yeung, C. H</au><au>Skupin, R</au><au>Haufe, G</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antifertility potential of ornidazole analogues in rats</atitle><jtitle>Journal of andrology</jtitle><addtitle>J Androl</addtitle><date>1997-07</date><risdate>1997</risdate><volume>18</volume><issue>4</issue><spage>431</spage><epage>438</epage><pages>431-438</pages><issn>0196-3635</issn><eissn>1939-4640</eissn><coden>JOAND3</coden><abstract>In order to determine which part of the ornidazole molecule [1‐(3‐chloro‐2‐hydroxy)propyhl‐2‐methyl‐5‐nitroimidazole] is responsible for its antifertility action, structural analogues were fed to male rats of proven fertility at doses equivalent to the antifertility dose of ornidazole (1.82 mmol/kg/day). The fertility of the males was tested, before oral gavage (control mating) and after 10 and 14 days of feeding, by counting the number of fetuses and corpora lutea present in females 12 days after mating. The day after the last mating, the kinematic parameters of sperm from the cauda epididymldis were assessed objectively with a Hamilton‐Thome motility analyzer. Analogues bearing the 2‐nitro and 5‐methyl groups on the imidazole ring were inactive if the (chlorohydroxy)propyl group were substituted by proton or methyl, hydroxyethyl, chloroethyl, or (sulfonylethyl)ethyl groups, indicating that the three‐carbon side chain of ornidazole was necessary for the antifertility action. Only ornidazole and its acetate were effective antifertility agents, but a compound bearing the (chlorohydroxy)propyi side chain attached to a nitrogen atom of a heterocyclic phthalimide produced a partial but temporary reduction in fertility. 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subjects | Animals Biological and medical sciences Birth control Body Weight - drug effects CASA contraception Contraceptive Agents, Male - pharmacology Epididymis fertility Fertility - drug effects Gynecology. Andrology. Obstetrics Hematocrit Male Medical sciences nitroimidazoles Organ Size - drug effects Ornidazole - analogs & derivatives Ornidazole - pharmacology Other methods of contraception. Sterilization Rats Rats, Sprague-Dawley sperm motility Sperm Motility - drug effects |
title | Antifertility potential of ornidazole analogues in rats |
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