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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
Main Authors: Al-Qirim, Tariq, Shattat, Ghassan, Sweidan, Kamal, El-Huneidi, Waseem, Sheikha, Ghassan Abu, Khalaf, Reema Abu, Hikmat, Suhair
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creator Al-Qirim, Tariq
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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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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 &lt;0.0001) and 4c′ (p &lt;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 &lt;0.001) and 4c′ (p &lt;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. 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KGaA, Weinheim</rights><rights>Copyright © 2012 WILEY-VCH Verlag GmbH &amp; Co. KGaA, Weinheim.</rights><rights>Copyright © 2012 WILEY-VCH Verlag GmbH &amp; 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 &lt;0.0001) and 4c′ (p &lt;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 &lt;0.001) and 4c′ (p &lt;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 ; 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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 &lt;0.0001) and 4c′ (p &lt;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 &lt;0.001) and 4c′ (p &lt;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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identifier ISSN: 0365-6233
ispartof Archiv der Pharmazie (Weinheim), 2012-05, Vol.345 (5), p.401-406
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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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