{"id":11386,"date":"2022-11-24T03:06:45","date_gmt":"2022-11-23T19:06:45","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11386"},"modified":"2022-11-24T03:06:45","modified_gmt":"2022-11-23T19:06:45","slug":"seki-kunios-team-published-research-in-chemical-pharmaceutical-bulletin-in-32-cas-890590-91-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11386","title":{"rendered":"Seki, Kunio&#8217;s team published research in Chemical &amp; Pharmaceutical Bulletin  in 32 | CAS: 890590-91-7"},"content":{"rendered":"<p>Seki, Kunio published the artcile<b><i>Studies on hypolipidemic agents.  II.  Synthesis and pharmacological properties of alkylpyrazole derivatives<\/i><\/b>,  <a href=\"https:\/\/www.ambeed.com\/products\/890590-91-7.html\">Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid<\/a>,  the publication is  Chemical &amp; Pharmaceutical Bulletin (1984), 32(4), 1568-77, database is CAplus and MEDLINE.<\/p>\n<p>Claisen condensation of MeCOR (R = C<sub>1<\/sub>-C<sub>17<\/sub> alkyl) with (CO<sub>2<\/sub>Et)<sub>2<\/sub> gave enolates RCOCH:C(ONa)CO<sub>2<\/sub>Et, which underwent cyclocondensation with R<sup>1<\/sup>NHNH<sub>2<\/sub>[R<sup>1<\/sup> = H, Me, (CH<sub>2<\/sub>)<em><sub>n<\/sub><\/em>Me, C<sub>6<\/sub>H<sub>4<\/sub>R<sup>2<\/sup>-4; R<sup>2<\/sup> = H, Me, Cl, OMe, NH<sub>2<\/sub>; <em>n<\/em> = 7, 9, 11] to give pyrazoles <strong>I<\/strong> (R<sup>3<\/sup> = CO<sub>2<\/sub>H, CO<sub>2<\/sub>Et). Reduction of <strong>I<\/strong> (same R, R<sup>1<\/sup> = H, R<sup>2<\/sup> = CO<sub>2<\/sub>Et) gave <strong>I<\/strong> (R<sup>3<\/sup> = CH<sub>2<\/sub>OH) and hydrolysis of <strong>I<\/strong> (R<sup>3<\/sup> = CO<sub>2<\/sub>Et) gave <strong>I<\/strong> (R = CO<sub>2<\/sub>H). The latter compounds were chlorinated and amidated to give <strong>I<\/strong> [same R, R<sup>1<\/sup> = H, R<sup>3<\/sup> = CONHR<sup>4<\/sup>, R<sup>4<\/sup> = CH<sub>2<\/sub>CH<sub>2<\/sub>OH, CH<sub>2<\/sub>CO<sub>2<\/sub>Et, CH(CHMeEt)CO<sub>2<\/sub>Et, H, Bu, decyl]. These pyrazoles (46 compounds) were evaluated for hypolipidemic activity in rats. Homologation of the C-5 alkyl chain led to marked increase in activity, but introduction of other substituents at other sites on the pyrazole ring failed to enhance the activity. The replacement of the pyrazole ring with an isoxazole ring resulted in a marked decrease in activity. <strong>I<\/strong> (R = tridecyl, R<sup>1<\/sup> = H, R<sup>2<\/sup> = CO<sub>2<\/sub>H) was as effective as clofibrate in lowering serum triglycerides and cholesterol in rats and showed fairly low toxicity with LD<sub>50<\/sub> = 10.0 g\/kg orally in mice.<\/p>\n<p>Chemical &amp; Pharmaceutical Bulletin published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C48H47FeP, <a href=\"https:\/\/www.ambeed.com\/products\/890590-91-7.html\">Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid<\/a>.<\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,<br \/><a href=\"Pyrazole - Wikipedia\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Chemical &amp; Pharmaceutical Bulletin published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C48H47FeP, <a href=\"https:\/\/www.ambeed.com\/products\/890590-91-7.html\">Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[800,131],"tags":[717],"class_list":["post-11386","post","type-post","status-publish","format-standard","hentry","category-890590-91-7","category-pyrazoles-derivatives","tag-m-w150-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Seki, Kunio&#039;s team published research in Chemical &amp; Pharmaceutical Bulletin in 32 | CAS: 890590-91-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Seki, Kunio published the artcileStudies on hypolipidemic agents. 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