Biologically active dihydropyrimidones of the Biginelli-type — a literature survey
In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1 H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received...
Gespeichert in:
| Veröffentlicht in: | European Journal of Medicinal Chemistry 2000-12, Vol.35 (12), p.1043-1052 |
|---|---|
| 1. Verfasser: | |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1052 |
|---|---|
| container_issue | 12 |
| container_start_page | 1043 |
| container_title | European Journal of Medicinal Chemistry |
| container_volume | 35 |
| creator | Kappe, C.Oliver |
| description | In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1
H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs recently developed as calcium channel modulators, α
1a adrenoceptor-selective antagonists and compounds that target the mitotic machinery. |
| doi_str_mv | 10.1016/S0223-5234(00)01189-2 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_72575365</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0223523400011892</els_id><sourcerecordid>72575365</sourcerecordid><originalsourceid>FETCH-LOGICAL-c455t-2fb1dc2fce887988825d5b65a1dda6c857f9857dca73a970aec2becb3ed97f5f3</originalsourceid><addsrcrecordid>eNqFkMtq3DAUhkVJaCaTPkKDIFDShVtJtix5FTpD2wQGuuhkLWTpaKLgsSaSPeBdHqJPmCeJ50K6zOaczfefy4fQZ0q-UULL738JY3nGWV5cE_KVUCqrjH1AEypKmeWMFydo8oacofOUHgkhvCTkIzqjlBWyIPkELWc-NGHljW6aAWvT-S1g6x8GG8NmiH7tbWgh4eBw9wB45le-habxWTdsAL88_8MaN76DqLs-Ak593MJwgU6dbhJ8OvYpuv_1czm_zRZ_ft_NfywyU3DeZczV1BrmDEgpKikl45bXJdfUWl0ayYWrxmKNFrmuBNFgWA2mzsFWwnGXT9GXw9xNDE89pE6tfTLjebqF0CclGBc8L_kI8gNoYkgpglOb8TUdB0WJ2ulUe51q50oRovY6FRtzl8cFfb0G-z919DcCV0dAp1Ghi7o1Pr1xshBC7MbcHCgYZWw9RJWMh9aA9RFMp2zw7xzyCgdjk68</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>72575365</pqid></control><display><type>article</type><title>Biologically active dihydropyrimidones of the Biginelli-type — a literature survey</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Kappe, C.Oliver</creator><creatorcontrib>Kappe, C.Oliver</creatorcontrib><description>In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1
H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs recently developed as calcium channel modulators, α
1a adrenoceptor-selective antagonists and compounds that target the mitotic machinery.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/S0223-5234(00)01189-2</identifier><identifier>PMID: 11248403</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Oxford: Elsevier Masson SAS</publisher><subject>Adrenergic alpha-1 Receptor Antagonists ; Adrenergic alpha-Antagonists - chemical synthesis ; Adrenergic alpha-Antagonists - chemistry ; Adrenergic alpha-Antagonists - pharmacology ; Antineoplastic agents ; benign prostatic hyperplasia ; Biological and medical sciences ; calcium channel modulators ; Calcium Channels - drug effects ; cardiovascular disease ; Cardiovascular system ; Catecholaminergic system ; dihydropyridines ; dihydropyrimidones ; General aspects ; Humans ; Kinesin - antagonists & inhibitors ; Medical sciences ; Miscellaneous ; Mitosis ; mitotic machinery ; Molecular Conformation ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Pyrimidinones - chemical synthesis ; Pyrimidinones - chemistry ; Pyrimidinones - pharmacology</subject><ispartof>European Journal of Medicinal Chemistry, 2000-12, Vol.35 (12), p.1043-1052</ispartof><rights>2000 Éditions scientifiques et médicales Elsevier SAS</rights><rights>2001 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c455t-2fb1dc2fce887988825d5b65a1dda6c857f9857dca73a970aec2becb3ed97f5f3</citedby><cites>FETCH-LOGICAL-c455t-2fb1dc2fce887988825d5b65a1dda6c857f9857dca73a970aec2becb3ed97f5f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0223523400011892$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>313,314,776,780,788,3536,27901,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=847772$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11248403$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kappe, C.Oliver</creatorcontrib><title>Biologically active dihydropyrimidones of the Biginelli-type — a literature survey</title><title>European Journal of Medicinal Chemistry</title><addtitle>Eur J Med Chem</addtitle><description>In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1
H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs recently developed as calcium channel modulators, α
1a adrenoceptor-selective antagonists and compounds that target the mitotic machinery.</description><subject>Adrenergic alpha-1 Receptor Antagonists</subject><subject>Adrenergic alpha-Antagonists - chemical synthesis</subject><subject>Adrenergic alpha-Antagonists - chemistry</subject><subject>Adrenergic alpha-Antagonists - pharmacology</subject><subject>Antineoplastic agents</subject><subject>benign prostatic hyperplasia</subject><subject>Biological and medical sciences</subject><subject>calcium channel modulators</subject><subject>Calcium Channels - drug effects</subject><subject>cardiovascular disease</subject><subject>Cardiovascular system</subject><subject>Catecholaminergic system</subject><subject>dihydropyridines</subject><subject>dihydropyrimidones</subject><subject>General aspects</subject><subject>Humans</subject><subject>Kinesin - antagonists & inhibitors</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Mitosis</subject><subject>mitotic machinery</subject><subject>Molecular Conformation</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrimidinones - chemical synthesis</subject><subject>Pyrimidinones - chemistry</subject><subject>Pyrimidinones - pharmacology</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMtq3DAUhkVJaCaTPkKDIFDShVtJtix5FTpD2wQGuuhkLWTpaKLgsSaSPeBdHqJPmCeJ50K6zOaczfefy4fQZ0q-UULL738JY3nGWV5cE_KVUCqrjH1AEypKmeWMFydo8oacofOUHgkhvCTkIzqjlBWyIPkELWc-NGHljW6aAWvT-S1g6x8GG8NmiH7tbWgh4eBw9wB45le-habxWTdsAL88_8MaN76DqLs-Ak593MJwgU6dbhJ8OvYpuv_1czm_zRZ_ft_NfywyU3DeZczV1BrmDEgpKikl45bXJdfUWl0ayYWrxmKNFrmuBNFgWA2mzsFWwnGXT9GXw9xNDE89pE6tfTLjebqF0CclGBc8L_kI8gNoYkgpglOb8TUdB0WJ2ulUe51q50oRovY6FRtzl8cFfb0G-z919DcCV0dAp1Ghi7o1Pr1xshBC7MbcHCgYZWw9RJWMh9aA9RFMp2zw7xzyCgdjk68</recordid><startdate>20001201</startdate><enddate>20001201</enddate><creator>Kappe, C.Oliver</creator><general>Elsevier Masson SAS</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>20001201</creationdate><title>Biologically active dihydropyrimidones of the Biginelli-type — a literature survey</title><author>Kappe, C.Oliver</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c455t-2fb1dc2fce887988825d5b65a1dda6c857f9857dca73a970aec2becb3ed97f5f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Adrenergic alpha-1 Receptor Antagonists</topic><topic>Adrenergic alpha-Antagonists - chemical synthesis</topic><topic>Adrenergic alpha-Antagonists - chemistry</topic><topic>Adrenergic alpha-Antagonists - pharmacology</topic><topic>Antineoplastic agents</topic><topic>benign prostatic hyperplasia</topic><topic>Biological and medical sciences</topic><topic>calcium channel modulators</topic><topic>Calcium Channels - drug effects</topic><topic>cardiovascular disease</topic><topic>Cardiovascular system</topic><topic>Catecholaminergic system</topic><topic>dihydropyridines</topic><topic>dihydropyrimidones</topic><topic>General aspects</topic><topic>Humans</topic><topic>Kinesin - antagonists & inhibitors</topic><topic>Medical sciences</topic><topic>Miscellaneous</topic><topic>Mitosis</topic><topic>mitotic machinery</topic><topic>Molecular Conformation</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrimidinones - chemical synthesis</topic><topic>Pyrimidinones - chemistry</topic><topic>Pyrimidinones - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kappe, C.Oliver</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>European Journal of Medicinal Chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kappe, C.Oliver</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biologically active dihydropyrimidones of the Biginelli-type — a literature survey</atitle><jtitle>European Journal of Medicinal Chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2000-12-01</date><risdate>2000</risdate><volume>35</volume><issue>12</issue><spage>1043</spage><epage>1052</epage><pages>1043-1052</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1
H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review, we highlight recent developments in this area, with a focus on the DHPMs recently developed as calcium channel modulators, α
1a adrenoceptor-selective antagonists and compounds that target the mitotic machinery.</abstract><cop>Oxford</cop><pub>Elsevier Masson SAS</pub><pmid>11248403</pmid><doi>10.1016/S0223-5234(00)01189-2</doi><tpages>10</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0223-5234 |
| ispartof | European Journal of Medicinal Chemistry, 2000-12, Vol.35 (12), p.1043-1052 |
| issn | 0223-5234 1768-3254 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_72575365 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists - chemical synthesis Adrenergic alpha-Antagonists - chemistry Adrenergic alpha-Antagonists - pharmacology Antineoplastic agents benign prostatic hyperplasia Biological and medical sciences calcium channel modulators Calcium Channels - drug effects cardiovascular disease Cardiovascular system Catecholaminergic system dihydropyridines dihydropyrimidones General aspects Humans Kinesin - antagonists & inhibitors Medical sciences Miscellaneous Mitosis mitotic machinery Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrimidinones - chemical synthesis Pyrimidinones - chemistry Pyrimidinones - pharmacology |
| title | Biologically active dihydropyrimidones of the Biginelli-type — a literature survey |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-25T19%3A59%3A57IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Biologically%20active%20dihydropyrimidones%20of%20the%20Biginelli-type%20%E2%80%94%20a%20literature%20survey&rft.jtitle=European%20Journal%20of%20Medicinal%20Chemistry&rft.au=Kappe,%20C.Oliver&rft.date=2000-12-01&rft.volume=35&rft.issue=12&rft.spage=1043&rft.epage=1052&rft.pages=1043-1052&rft.issn=0223-5234&rft.eissn=1768-3254&rft.coden=EJMCA5&rft_id=info:doi/10.1016/S0223-5234(00)01189-2&rft_dat=%3Cproquest_cross%3E72575365%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=72575365&rft_id=info:pmid/11248403&rft_els_id=S0223523400011892&rfr_iscdi=true |