Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers
[Display omitted] N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2018-02, Vol.26 (3), p.603-608 |
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| container_issue | 3 |
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| container_title | Bioorganic & medicinal chemistry |
| container_volume | 26 |
| creator | Kumamoto, Takuya Nakajima, Marie Uga, Reina Ihayazaka, Naoko Kashihara, Haruna Katakawa, Kazuaki Ishikawa, Tsutomu Saiki, Ryotaro Nishimura, Kazuhiro Igarashi, Kazuei |
| description | [Display omitted]
N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine. |
| doi_str_mv | 10.1016/j.bmc.2017.12.021 |
| format | Article |
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N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2017.12.021</identifier><identifier>PMID: 29277306</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Alzheimer’s disease ; Guanidine ; Memantine ; NMDA channel blocker ; Polyamine</subject><ispartof>Bioorganic & medicinal chemistry, 2018-02, Vol.26 (3), p.603-608</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c419t-172ecb4f84640b97fb5a5d40eb0dedac00ea32d1aed41cbff14969968a54fb4f3</citedby><cites>FETCH-LOGICAL-c419t-172ecb4f84640b97fb5a5d40eb0dedac00ea32d1aed41cbff14969968a54fb4f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2017.12.021$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29277306$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumamoto, Takuya</creatorcontrib><creatorcontrib>Nakajima, Marie</creatorcontrib><creatorcontrib>Uga, Reina</creatorcontrib><creatorcontrib>Ihayazaka, Naoko</creatorcontrib><creatorcontrib>Kashihara, Haruna</creatorcontrib><creatorcontrib>Katakawa, Kazuaki</creatorcontrib><creatorcontrib>Ishikawa, Tsutomu</creatorcontrib><creatorcontrib>Saiki, Ryotaro</creatorcontrib><creatorcontrib>Nishimura, Kazuhiro</creatorcontrib><creatorcontrib>Igarashi, Kazuei</creatorcontrib><title>Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.</description><subject>Alzheimer’s disease</subject><subject>Guanidine</subject><subject>Memantine</subject><subject>NMDA channel blocker</subject><subject>Polyamine</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><recordid>eNp9kE9v1DAQxS0EokvhA3BBPnJo0hnHSdbiVLVAK5X2AgdOlv9MWC-Js9jZSvvtcbWFY0_zDu89zfsx9h6hRsDufFvbydUCsK9R1CDwBVuh7GTVNApfshWobl3BWnUn7E3OWwAQUuFrdiKU6PsGuhX7eUU5_IpnPB_isik6n3ETPacHM-7NEubI54Hv5vFgphCpmmgycSmKbw42BZ-5yfzu29UFdxsTI43cjrP7TSm_Za8GM2Z693RP2Y8vn79fXle3919vLi9uKydRLRX2gpyVw7r8DVb1g21N6yWQBU_eOAAyjfBoyEt0dhhQqk6VYaaVQ8k1p-zjsXeX5j97youeQnY0jibSvM8a1RraFrETxYpHq0tzzokGvUthMumgEfQjUb3Vhah-JKpR6EK0ZD481e_tRP5_4h_CYvh0NFAZ-RAo6ewCRUc-JHKL9nN4pv4vkKKHVA</recordid><startdate>20180201</startdate><enddate>20180201</enddate><creator>Kumamoto, Takuya</creator><creator>Nakajima, Marie</creator><creator>Uga, Reina</creator><creator>Ihayazaka, Naoko</creator><creator>Kashihara, Haruna</creator><creator>Katakawa, Kazuaki</creator><creator>Ishikawa, Tsutomu</creator><creator>Saiki, Ryotaro</creator><creator>Nishimura, Kazuhiro</creator><creator>Igarashi, Kazuei</creator><general>Elsevier Ltd</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20180201</creationdate><title>Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers</title><author>Kumamoto, Takuya ; Nakajima, Marie ; Uga, Reina ; Ihayazaka, Naoko ; Kashihara, Haruna ; Katakawa, Kazuaki ; Ishikawa, Tsutomu ; Saiki, Ryotaro ; Nishimura, Kazuhiro ; Igarashi, Kazuei</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c419t-172ecb4f84640b97fb5a5d40eb0dedac00ea32d1aed41cbff14969968a54fb4f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Alzheimer’s disease</topic><topic>Guanidine</topic><topic>Memantine</topic><topic>NMDA channel blocker</topic><topic>Polyamine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumamoto, Takuya</creatorcontrib><creatorcontrib>Nakajima, Marie</creatorcontrib><creatorcontrib>Uga, Reina</creatorcontrib><creatorcontrib>Ihayazaka, Naoko</creatorcontrib><creatorcontrib>Kashihara, Haruna</creatorcontrib><creatorcontrib>Katakawa, Kazuaki</creatorcontrib><creatorcontrib>Ishikawa, Tsutomu</creatorcontrib><creatorcontrib>Saiki, Ryotaro</creatorcontrib><creatorcontrib>Nishimura, Kazuhiro</creatorcontrib><creatorcontrib>Igarashi, Kazuei</creatorcontrib><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>Kumamoto, Takuya</au><au>Nakajima, Marie</au><au>Uga, Reina</au><au>Ihayazaka, Naoko</au><au>Kashihara, Haruna</au><au>Katakawa, Kazuaki</au><au>Ishikawa, Tsutomu</au><au>Saiki, Ryotaro</au><au>Nishimura, Kazuhiro</au><au>Igarashi, Kazuei</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2018-02-01</date><risdate>2018</risdate><volume>26</volume><issue>3</issue><spage>603</spage><epage>608</epage><pages>603-608</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>29277306</pmid><doi>10.1016/j.bmc.2017.12.021</doi><tpages>6</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry, 2018-02, Vol.26 (3), p.603-608 |
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| language | eng |
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| source | Access via ScienceDirect (Elsevier) |
| subjects | Alzheimer’s disease Guanidine Memantine NMDA channel blocker Polyamine |
| title | Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers |
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