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In Vivo Antihyperlipidemic Activity of a New Series of N-(Benzoylphenyl) and N-(Acetylphenyl)-1-benzofuran-2-carboxamides in Rats
A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized. Compounds (3a, 3b, and 4a′–4c′) were tested in vivo using Triton‐WR‐1339‐induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals...
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Published in: | Archiv der Pharmazie (Weinheim) 2012-05, Vol.345 (5), p.401-406 |
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creator | Al-Qirim, Tariq Shattat, Ghassan Sweidan, Kamal El-Huneidi, Waseem Sheikha, Ghassan Abu Khalaf, Reema Abu Hikmat, Suhair |
description | A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized. Compounds (3a, 3b, and 4a′–4c′) were tested in vivo using Triton‐WR‐1339‐induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals were divided into eight groups: control, hyperlipidemic, 3a, 3b, 4a′, 4b′, 4c′, and bezafibrate. At a dose of 15 mg/kg, the elevated plasma triglyceride (TG) levels were significantly reduced in compounds 3b (p |
doi_str_mv | 10.1002/ardp.201100225 |
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A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized and most of them were tested in vivo for their hypolipidemic activity. Compounds 3b and 4c′ turned out to be potent lipid‐lowering agents and thus may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.</description><identifier>ISSN: 0365-6233</identifier><identifier>EISSN: 1521-4184</identifier><identifier>DOI: 10.1002/ardp.201100225</identifier><identifier>PMID: 22266816</identifier><language>eng</language><publisher>Weinheim: WILEY-VCH Verlag</publisher><subject>Animals ; Benzofurans - chemical synthesis ; Benzofurans - pharmacology ; Bezafibrate - pharmacology ; Cholesterol ; Cholesterol, HDL - blood ; Cholesterol, LDL - blood ; High-density lipoprotein-cholesterol ; Hypolipidemic activity ; Hypolipidemic Agents - chemical synthesis ; Hypolipidemic Agents - pharmacology ; Male ; Medical research ; N-(Benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides ; Polyethylene Glycols ; Rats ; Rats, Wistar ; Structure-Activity Relationship ; Triglycerides ; Triglycerides - blood ; Triton-induced hyperlipidemia</subject><ispartof>Archiv der Pharmazie (Weinheim), 2012-05, Vol.345 (5), p.401-406</ispartof><rights>Copyright © 2012 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.</rights><rights>Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4775-aa6c47181339922085bcdf239bb3992eac1049c7efc89e0dcec1096790b423083</citedby><cites>FETCH-LOGICAL-c4775-aa6c47181339922085bcdf239bb3992eac1049c7efc89e0dcec1096790b423083</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22266816$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Al-Qirim, Tariq</creatorcontrib><creatorcontrib>Shattat, Ghassan</creatorcontrib><creatorcontrib>Sweidan, Kamal</creatorcontrib><creatorcontrib>El-Huneidi, Waseem</creatorcontrib><creatorcontrib>Sheikha, Ghassan Abu</creatorcontrib><creatorcontrib>Khalaf, Reema Abu</creatorcontrib><creatorcontrib>Hikmat, Suhair</creatorcontrib><title>In Vivo Antihyperlipidemic Activity of a New Series of N-(Benzoylphenyl) and N-(Acetylphenyl)-1-benzofuran-2-carboxamides in Rats</title><title>Archiv der Pharmazie (Weinheim)</title><addtitle>Arch. Pharm. Pharm. Med. Chem</addtitle><description>A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized. Compounds (3a, 3b, and 4a′–4c′) were tested in vivo using Triton‐WR‐1339‐induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals were divided into eight groups: control, hyperlipidemic, 3a, 3b, 4a′, 4b′, 4c′, and bezafibrate. At a dose of 15 mg/kg, the elevated plasma triglyceride (TG) levels were significantly reduced in compounds 3b (p <0.0001) and 4c′ (p <0.05) after 12 and 24 h compared to the normal control group. Furthermore, high‐density lipoprotein‐cholesterol levels were remarkably increased in compounds 3b (p <0.001) and 4c′ (p <0.05). Meanwhile, compound 4b′ slightly reduced the TG levels after 12 and 24 h. The present study demonstrated new properties of the novel series of benzofuran‐2‐carboxamides 3b and 4c′ as potent lipid‐lowering agents. It is, therefore, reasonable to assume that compounds 3b and 4c′ may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.
A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized and most of them were tested in vivo for their hypolipidemic activity. Compounds 3b and 4c′ turned out to be potent lipid‐lowering agents and thus may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.</description><subject>Animals</subject><subject>Benzofurans - chemical synthesis</subject><subject>Benzofurans - pharmacology</subject><subject>Bezafibrate - pharmacology</subject><subject>Cholesterol</subject><subject>Cholesterol, HDL - blood</subject><subject>Cholesterol, LDL - blood</subject><subject>High-density lipoprotein-cholesterol</subject><subject>Hypolipidemic activity</subject><subject>Hypolipidemic Agents - chemical synthesis</subject><subject>Hypolipidemic Agents - pharmacology</subject><subject>Male</subject><subject>Medical research</subject><subject>N-(Benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides</subject><subject>Polyethylene Glycols</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Structure-Activity Relationship</subject><subject>Triglycerides</subject><subject>Triglycerides - blood</subject><subject>Triton-induced hyperlipidemia</subject><issn>0365-6233</issn><issn>1521-4184</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><recordid>eNqFkUtv1DAUhS0EokPLliWyxKYsPPgR57FMB2iLqqEMhbKzHOdGdUmcYCdt0x3_nERTRohNV_feo-8cWzoIvWJ0ySjl77QvuyWnbD64fIIWTHJGIpZGT9GCiliSmAuxh16EcE0pFZTL52iPcx7HKYsX6Pepw9_tTYtz19ursQNf286W0FiDc9PbG9uPuK2wxmu4xV_BWwjzvSaHR-Du27HursCN9VusXTmruYF-JxJGipmqBq8d4cRoX7R3upkeCNg6vNF9OEDPKl0HePkw99G3jx8uVifk7PPx6So_IyZKEkm0jqeFpUyILOOcprIwZcVFVhSzANowGmUmgcqkGdDSwCRkcZLRIuKCpmIfHW5zO9_-GiD0qrHBQF1rB-0QFKNM0kwwNqNv_kOv28G76XeKyShKk1RGyUQtt5TxbQgeKtV522g_TlFq7kPN5ahdOZPh9UPsUDRQ7vC_bUxAtgVubQ3jI3Eq37w__zecbL029HC382r_U8WJSKS6XB-rHxu6uvj05VKdiz8EAqlZ</recordid><startdate>201205</startdate><enddate>201205</enddate><creator>Al-Qirim, Tariq</creator><creator>Shattat, Ghassan</creator><creator>Sweidan, Kamal</creator><creator>El-Huneidi, Waseem</creator><creator>Sheikha, Ghassan Abu</creator><creator>Khalaf, Reema Abu</creator><creator>Hikmat, Suhair</creator><general>WILEY-VCH Verlag</general><general>WILEY‐VCH Verlag</general><general>Wiley Subscription Services, Inc</general><scope>BSCLL</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>K9.</scope><scope>7X8</scope></search><sort><creationdate>201205</creationdate><title>In Vivo Antihyperlipidemic Activity of a New Series of N-(Benzoylphenyl) and N-(Acetylphenyl)-1-benzofuran-2-carboxamides in Rats</title><author>Al-Qirim, Tariq ; Shattat, Ghassan ; Sweidan, Kamal ; El-Huneidi, Waseem ; Sheikha, Ghassan Abu ; Khalaf, Reema Abu ; Hikmat, Suhair</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4775-aa6c47181339922085bcdf239bb3992eac1049c7efc89e0dcec1096790b423083</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Animals</topic><topic>Benzofurans - chemical synthesis</topic><topic>Benzofurans - pharmacology</topic><topic>Bezafibrate - pharmacology</topic><topic>Cholesterol</topic><topic>Cholesterol, HDL - blood</topic><topic>Cholesterol, LDL - blood</topic><topic>High-density lipoprotein-cholesterol</topic><topic>Hypolipidemic activity</topic><topic>Hypolipidemic Agents - chemical synthesis</topic><topic>Hypolipidemic Agents - pharmacology</topic><topic>Male</topic><topic>Medical research</topic><topic>N-(Benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides</topic><topic>Polyethylene Glycols</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Structure-Activity Relationship</topic><topic>Triglycerides</topic><topic>Triglycerides - blood</topic><topic>Triton-induced hyperlipidemia</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Al-Qirim, Tariq</creatorcontrib><creatorcontrib>Shattat, Ghassan</creatorcontrib><creatorcontrib>Sweidan, Kamal</creatorcontrib><creatorcontrib>El-Huneidi, Waseem</creatorcontrib><creatorcontrib>Sheikha, Ghassan Abu</creatorcontrib><creatorcontrib>Khalaf, Reema Abu</creatorcontrib><creatorcontrib>Hikmat, Suhair</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>MEDLINE - Academic</collection><jtitle>Archiv der Pharmazie (Weinheim)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Al-Qirim, Tariq</au><au>Shattat, Ghassan</au><au>Sweidan, Kamal</au><au>El-Huneidi, Waseem</au><au>Sheikha, Ghassan Abu</au><au>Khalaf, Reema Abu</au><au>Hikmat, Suhair</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In Vivo Antihyperlipidemic Activity of a New Series of N-(Benzoylphenyl) and N-(Acetylphenyl)-1-benzofuran-2-carboxamides in Rats</atitle><jtitle>Archiv der Pharmazie (Weinheim)</jtitle><addtitle>Arch. Pharm. Pharm. Med. Chem</addtitle><date>2012-05</date><risdate>2012</risdate><volume>345</volume><issue>5</issue><spage>401</spage><epage>406</epage><pages>401-406</pages><issn>0365-6233</issn><eissn>1521-4184</eissn><abstract>A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized. Compounds (3a, 3b, and 4a′–4c′) were tested in vivo using Triton‐WR‐1339‐induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals were divided into eight groups: control, hyperlipidemic, 3a, 3b, 4a′, 4b′, 4c′, and bezafibrate. At a dose of 15 mg/kg, the elevated plasma triglyceride (TG) levels were significantly reduced in compounds 3b (p <0.0001) and 4c′ (p <0.05) after 12 and 24 h compared to the normal control group. Furthermore, high‐density lipoprotein‐cholesterol levels were remarkably increased in compounds 3b (p <0.001) and 4c′ (p <0.05). Meanwhile, compound 4b′ slightly reduced the TG levels after 12 and 24 h. The present study demonstrated new properties of the novel series of benzofuran‐2‐carboxamides 3b and 4c′ as potent lipid‐lowering agents. It is, therefore, reasonable to assume that compounds 3b and 4c′ may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.
A new series of N‐(benzoylphenyl) and N‐(acetylphenyl)‐1‐benzofuran‐2‐carboxamides (3a–3d and 4a′–4c′) were synthesized and most of them were tested in vivo for their hypolipidemic activity. Compounds 3b and 4c′ turned out to be potent lipid‐lowering agents and thus may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.</abstract><cop>Weinheim</cop><pub>WILEY-VCH Verlag</pub><pmid>22266816</pmid><doi>10.1002/ardp.201100225</doi><tpages>6</tpages></addata></record> |
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subjects | Animals Benzofurans - chemical synthesis Benzofurans - pharmacology Bezafibrate - pharmacology Cholesterol Cholesterol, HDL - blood Cholesterol, LDL - blood High-density lipoprotein-cholesterol Hypolipidemic activity Hypolipidemic Agents - chemical synthesis Hypolipidemic Agents - pharmacology Male Medical research N-(Benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides Polyethylene Glycols Rats Rats, Wistar Structure-Activity Relationship Triglycerides Triglycerides - blood Triton-induced hyperlipidemia |
title | In Vivo Antihyperlipidemic Activity of a New Series of N-(Benzoylphenyl) and N-(Acetylphenyl)-1-benzofuran-2-carboxamides in Rats |
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