Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents
A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipi...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2010-06, Vol.18 (11), p.4138-4148 |
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| container_issue | 11 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Kumar, Atul Sharma, Siddharth Tripathi, Vishwa Deepak Maurya, Ram Awatar Srivastava, Swayam Prakash Bhatia, Gitika Tamrakar, A.K. Srivastava, Arvind Kumar |
| description | A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipid and TG modulating activity. All these compounds were evaluated in various in vitro models of diabetes to know the possible mechanism of their antihyperglycemic action. Interestingly, compounds
3a–r (diaryl substitution
) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds
5a–
d (acid substituted) have shown significant glycogen phosphorylase activity. |
| doi_str_mv | 10.1016/j.bmc.2009.11.061 |
| format | Article |
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3a–r (diaryl substitution
) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds
5a–
d (acid substituted) have shown significant glycogen phosphorylase activity.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2009.11.061</identifier><identifier>PMID: 20471838</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Animals ; Antidyslipidemic ; Antihyperglcemic ; Biological and medical sciences ; Diabetes Mellitus, Experimental - drug therapy ; Drug Design ; Dyslipidemias - drug therapy ; General and cellular metabolism. Vitamins ; Glycogen phosphorylase ; Glycogen Phosphorylase - antagonists & inhibitors ; Hypoglycemic Agents - chemical synthesis ; Hypoglycemic Agents - pharmacology ; Medical sciences ; Mice ; Mice, Inbred Strains ; Pharmacology. Drug treatments ; Polyhydroquinoline ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors ; PTP-1B ; Quinolines - chemical synthesis ; Quinolines - pharmacology</subject><ispartof>Bioorganic & medicinal chemistry, 2010-06, Vol.18 (11), p.4138-4148</ispartof><rights>2009</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c382t-7e54ca4e3cd93add9d3d7976d5a13634b87fa5b318d02291eafdcbd32f55ee953</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2009.11.061$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22902277$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20471838$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumar, Atul</creatorcontrib><creatorcontrib>Sharma, Siddharth</creatorcontrib><creatorcontrib>Tripathi, Vishwa Deepak</creatorcontrib><creatorcontrib>Maurya, Ram Awatar</creatorcontrib><creatorcontrib>Srivastava, Swayam Prakash</creatorcontrib><creatorcontrib>Bhatia, Gitika</creatorcontrib><creatorcontrib>Tamrakar, A.K.</creatorcontrib><creatorcontrib>Srivastava, Arvind Kumar</creatorcontrib><title>Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipid and TG modulating activity. All these compounds were evaluated in various in vitro models of diabetes to know the possible mechanism of their antihyperglycemic action. Interestingly, compounds
3a–r (diaryl substitution
) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds
5a–
d (acid substituted) have shown significant glycogen phosphorylase activity.</description><subject>Animals</subject><subject>Antidyslipidemic</subject><subject>Antihyperglcemic</subject><subject>Biological and medical sciences</subject><subject>Diabetes Mellitus, Experimental - drug therapy</subject><subject>Drug Design</subject><subject>Dyslipidemias - drug therapy</subject><subject>General and cellular metabolism. Vitamins</subject><subject>Glycogen phosphorylase</subject><subject>Glycogen Phosphorylase - antagonists & inhibitors</subject><subject>Hypoglycemic Agents - chemical synthesis</subject><subject>Hypoglycemic Agents - pharmacology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred Strains</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyhydroquinoline</subject><subject>Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors</subject><subject>PTP-1B</subject><subject>Quinolines - chemical synthesis</subject><subject>Quinolines - pharmacology</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kD2P1DAQhi0E4vYOfgANSoNoSPDY-bKo0MEB0kk0UFuOPdn1KnFCxjkp_Hq87AId1WikZ1698zD2AngBHOq3x6IbbSE4VwVAwWt4xHZQ1mUupYLHbMdV3ea8VfUVuyY6cs5FqeApuxK8bKCV7Y79_IDk9yEzwWW0hXhIK2VTn4k3Ze48rR1FH9eILpunYTtsbpl-rD5Mgw9ImaFsXiaa0Ub_gCkl-sM247IfNoujt79zBz97l42TWwcTfdhnZo8h0jP2pDcD4fPLvGHf7z5-u_2c33_99OX2_X1uZSti3mBVWlOitE5J45xy0jWqqV1lQNay7NqmN1UnoXVcCAVoemc7J0VfVYiqkjfs9Tl3PlVHinr0ZHEYTMBpJd1ICaKSJSQSzqRNP9GCvZ4XP5pl08D1ybg-6mRcn4xrAJ2Mp5uXl_S1G9H9vfijOAGvLoAha4Z-McF6-scJlWo3TeLenTlMLh48Lpqsx2DR-SXp1W7y_6nxC4nioa0</recordid><startdate>20100601</startdate><enddate>20100601</enddate><creator>Kumar, Atul</creator><creator>Sharma, Siddharth</creator><creator>Tripathi, Vishwa Deepak</creator><creator>Maurya, Ram Awatar</creator><creator>Srivastava, Swayam Prakash</creator><creator>Bhatia, Gitika</creator><creator>Tamrakar, A.K.</creator><creator>Srivastava, Arvind Kumar</creator><general>Elsevier Ltd</general><general>Elsevier</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>20100601</creationdate><title>Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents</title><author>Kumar, Atul ; Sharma, Siddharth ; Tripathi, Vishwa Deepak ; Maurya, Ram Awatar ; Srivastava, Swayam Prakash ; Bhatia, Gitika ; Tamrakar, A.K. ; Srivastava, Arvind Kumar</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c382t-7e54ca4e3cd93add9d3d7976d5a13634b87fa5b318d02291eafdcbd32f55ee953</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Animals</topic><topic>Antidyslipidemic</topic><topic>Antihyperglcemic</topic><topic>Biological and medical sciences</topic><topic>Diabetes Mellitus, Experimental - drug therapy</topic><topic>Drug Design</topic><topic>Dyslipidemias - drug therapy</topic><topic>General and cellular metabolism. Vitamins</topic><topic>Glycogen phosphorylase</topic><topic>Glycogen Phosphorylase - antagonists & inhibitors</topic><topic>Hypoglycemic Agents - chemical synthesis</topic><topic>Hypoglycemic Agents - pharmacology</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred Strains</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyhydroquinoline</topic><topic>Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors</topic><topic>PTP-1B</topic><topic>Quinolines - chemical synthesis</topic><topic>Quinolines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumar, Atul</creatorcontrib><creatorcontrib>Sharma, Siddharth</creatorcontrib><creatorcontrib>Tripathi, Vishwa Deepak</creatorcontrib><creatorcontrib>Maurya, Ram Awatar</creatorcontrib><creatorcontrib>Srivastava, Swayam Prakash</creatorcontrib><creatorcontrib>Bhatia, Gitika</creatorcontrib><creatorcontrib>Tamrakar, A.K.</creatorcontrib><creatorcontrib>Srivastava, Arvind Kumar</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>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kumar, Atul</au><au>Sharma, Siddharth</au><au>Tripathi, Vishwa Deepak</au><au>Maurya, Ram Awatar</au><au>Srivastava, Swayam Prakash</au><au>Bhatia, Gitika</au><au>Tamrakar, A.K.</au><au>Srivastava, Arvind Kumar</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2010-06-01</date><risdate>2010</risdate><volume>18</volume><issue>11</issue><spage>4138</spage><epage>4148</epage><pages>4138-4148</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipid and TG modulating activity. All these compounds were evaluated in various in vitro models of diabetes to know the possible mechanism of their antihyperglycemic action. Interestingly, compounds
3a–r (diaryl substitution
) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds
5a–
d (acid substituted) have shown significant glycogen phosphorylase activity.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>20471838</pmid><doi>10.1016/j.bmc.2009.11.061</doi><tpages>11</tpages></addata></record> |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Antidyslipidemic Antihyperglcemic Biological and medical sciences Diabetes Mellitus, Experimental - drug therapy Drug Design Dyslipidemias - drug therapy General and cellular metabolism. Vitamins Glycogen phosphorylase Glycogen Phosphorylase - antagonists & inhibitors Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - pharmacology Medical sciences Mice Mice, Inbred Strains Pharmacology. Drug treatments Polyhydroquinoline Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors PTP-1B Quinolines - chemical synthesis Quinolines - pharmacology |
| title | Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents |
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