Pyrimidine derivatives with antitubercular activity
Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug d...
Gespeichert in:
| Veröffentlicht in: | European journal of medicinal chemistry 2023-01, Vol.246, p.114946-114946, Article 114946 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 114946 |
|---|---|
| container_issue | |
| container_start_page | 114946 |
| container_title | European journal of medicinal chemistry |
| container_volume | 246 |
| creator | Finger, Vladimir Kufa, Martin Soukup, Ondrej Castagnolo, Daniele Roh, Jaroslav Korabecny, Jan |
| description | Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.
[Display omitted]
•Pyrimidine represents a valuable scaffold in the discovery of antitubercular agents.•There are currently investigated three clinical candidates with pyrimidine core.•Pyrimidine-based drugs are sub-classified according to their mechanism of action. |
| doi_str_mv | 10.1016/j.ejmech.2022.114946 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_2746395787</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0223523422008480</els_id><sourcerecordid>2746395787</sourcerecordid><originalsourceid>FETCH-LOGICAL-c408t-8fb82c347f2f49c20f0483329c7af3f86aa1c84f789cfb1ea1feb841de5098c53</originalsourceid><addsrcrecordid>eNp9kMtOwzAURC0EoqXwBwh1ySbBz8TZIKGKl1QJFrC2HOdadZRHsZ2i_j2pUliyuouZuaM5CF0TnBJMsrs6hboFs0kppjQlhBc8O0FzkmcyYVTwUzQfBZYIyvgMXYRQY4xFhvE5mrGMiyIXxRyx9713ratcB8sKvNvp6HYQlt8ubpa6iy4OJXgzNNovtRk1F_eX6MzqJsDV8S7Q59Pjx-olWb89v64e1onhWMZE2lJSw3huqeWFodhiLhmjhcm1ZVZmWhMjuc1lYWxJQBMLpeSkAoELaQRboNvp79b3XwOEqFoXDDSN7qAfgqI5z1ghcpmPVj5Zje9D8GDVdpyl_V4RrA64VK0mXOqAS024xtjNsWEoW6j-Qr98RsP9ZIBx586BV8E46AxUzoOJqurd_w0_kzB9ig</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2746395787</pqid></control><display><type>article</type><title>Pyrimidine derivatives with antitubercular activity</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Finger, Vladimir ; Kufa, Martin ; Soukup, Ondrej ; Castagnolo, Daniele ; Roh, Jaroslav ; Korabecny, Jan</creator><creatorcontrib>Finger, Vladimir ; Kufa, Martin ; Soukup, Ondrej ; Castagnolo, Daniele ; Roh, Jaroslav ; Korabecny, Jan</creatorcontrib><description>Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.
[Display omitted]
•Pyrimidine represents a valuable scaffold in the discovery of antitubercular agents.•There are currently investigated three clinical candidates with pyrimidine core.•Pyrimidine-based drugs are sub-classified according to their mechanism of action.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2022.114946</identifier><identifier>PMID: 36459759</identifier><language>eng</language><publisher>France: Elsevier Masson SAS</publisher><subject>Antitubercular Agents - chemistry ; Drug development ; Drug Discovery ; Mycobacterium tuberculosis ; Pyrimidine ; Pyrimidines - pharmacology ; Structure-Activity Relationship ; Structure-activity relationships ; Tuberculosis</subject><ispartof>European journal of medicinal chemistry, 2023-01, Vol.246, p.114946-114946, Article 114946</ispartof><rights>2022 Elsevier Masson SAS</rights><rights>Copyright © 2022 Elsevier Masson SAS. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c408t-8fb82c347f2f49c20f0483329c7af3f86aa1c84f789cfb1ea1feb841de5098c53</citedby><cites>FETCH-LOGICAL-c408t-8fb82c347f2f49c20f0483329c7af3f86aa1c84f789cfb1ea1feb841de5098c53</cites><orcidid>0000-0003-4698-8379 ; 0000-0001-6977-7596</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0223523422008480$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/36459759$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Finger, Vladimir</creatorcontrib><creatorcontrib>Kufa, Martin</creatorcontrib><creatorcontrib>Soukup, Ondrej</creatorcontrib><creatorcontrib>Castagnolo, Daniele</creatorcontrib><creatorcontrib>Roh, Jaroslav</creatorcontrib><creatorcontrib>Korabecny, Jan</creatorcontrib><title>Pyrimidine derivatives with antitubercular activity</title><title>European journal of medicinal chemistry</title><addtitle>Eur J Med Chem</addtitle><description>Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.
[Display omitted]
•Pyrimidine represents a valuable scaffold in the discovery of antitubercular agents.•There are currently investigated three clinical candidates with pyrimidine core.•Pyrimidine-based drugs are sub-classified according to their mechanism of action.</description><subject>Antitubercular Agents - chemistry</subject><subject>Drug development</subject><subject>Drug Discovery</subject><subject>Mycobacterium tuberculosis</subject><subject>Pyrimidine</subject><subject>Pyrimidines - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Structure-activity relationships</subject><subject>Tuberculosis</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtOwzAURC0EoqXwBwh1ySbBz8TZIKGKl1QJFrC2HOdadZRHsZ2i_j2pUliyuouZuaM5CF0TnBJMsrs6hboFs0kppjQlhBc8O0FzkmcyYVTwUzQfBZYIyvgMXYRQY4xFhvE5mrGMiyIXxRyx9713ratcB8sKvNvp6HYQlt8ubpa6iy4OJXgzNNovtRk1F_eX6MzqJsDV8S7Q59Pjx-olWb89v64e1onhWMZE2lJSw3huqeWFodhiLhmjhcm1ZVZmWhMjuc1lYWxJQBMLpeSkAoELaQRboNvp79b3XwOEqFoXDDSN7qAfgqI5z1ghcpmPVj5Zje9D8GDVdpyl_V4RrA64VK0mXOqAS024xtjNsWEoW6j-Qr98RsP9ZIBx586BV8E46AxUzoOJqurd_w0_kzB9ig</recordid><startdate>20230115</startdate><enddate>20230115</enddate><creator>Finger, Vladimir</creator><creator>Kufa, Martin</creator><creator>Soukup, Ondrej</creator><creator>Castagnolo, Daniele</creator><creator>Roh, Jaroslav</creator><creator>Korabecny, Jan</creator><general>Elsevier Masson SAS</general><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><orcidid>https://orcid.org/0000-0003-4698-8379</orcidid><orcidid>https://orcid.org/0000-0001-6977-7596</orcidid></search><sort><creationdate>20230115</creationdate><title>Pyrimidine derivatives with antitubercular activity</title><author>Finger, Vladimir ; Kufa, Martin ; Soukup, Ondrej ; Castagnolo, Daniele ; Roh, Jaroslav ; Korabecny, Jan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c408t-8fb82c347f2f49c20f0483329c7af3f86aa1c84f789cfb1ea1feb841de5098c53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Antitubercular Agents - chemistry</topic><topic>Drug development</topic><topic>Drug Discovery</topic><topic>Mycobacterium tuberculosis</topic><topic>Pyrimidine</topic><topic>Pyrimidines - pharmacology</topic><topic>Structure-Activity Relationship</topic><topic>Structure-activity relationships</topic><topic>Tuberculosis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Finger, Vladimir</creatorcontrib><creatorcontrib>Kufa, Martin</creatorcontrib><creatorcontrib>Soukup, Ondrej</creatorcontrib><creatorcontrib>Castagnolo, Daniele</creatorcontrib><creatorcontrib>Roh, Jaroslav</creatorcontrib><creatorcontrib>Korabecny, Jan</creatorcontrib><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>Finger, Vladimir</au><au>Kufa, Martin</au><au>Soukup, Ondrej</au><au>Castagnolo, Daniele</au><au>Roh, Jaroslav</au><au>Korabecny, Jan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pyrimidine derivatives with antitubercular activity</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2023-01-15</date><risdate>2023</risdate><volume>246</volume><spage>114946</spage><epage>114946</epage><pages>114946-114946</pages><artnum>114946</artnum><issn>0223-5234</issn><eissn>1768-3254</eissn><abstract>Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.
[Display omitted]
•Pyrimidine represents a valuable scaffold in the discovery of antitubercular agents.•There are currently investigated three clinical candidates with pyrimidine core.•Pyrimidine-based drugs are sub-classified according to their mechanism of action.</abstract><cop>France</cop><pub>Elsevier Masson SAS</pub><pmid>36459759</pmid><doi>10.1016/j.ejmech.2022.114946</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0003-4698-8379</orcidid><orcidid>https://orcid.org/0000-0001-6977-7596</orcidid><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0223-5234 |
| ispartof | European journal of medicinal chemistry, 2023-01, Vol.246, p.114946-114946, Article 114946 |
| issn | 0223-5234 1768-3254 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_2746395787 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Antitubercular Agents - chemistry Drug development Drug Discovery Mycobacterium tuberculosis Pyrimidine Pyrimidines - pharmacology Structure-Activity Relationship Structure-activity relationships Tuberculosis |
| title | Pyrimidine derivatives with antitubercular activity |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-26T12%3A34%3A29IST&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=Pyrimidine%20derivatives%20with%20antitubercular%20activity&rft.jtitle=European%20journal%20of%20medicinal%20chemistry&rft.au=Finger,%20Vladimir&rft.date=2023-01-15&rft.volume=246&rft.spage=114946&rft.epage=114946&rft.pages=114946-114946&rft.artnum=114946&rft.issn=0223-5234&rft.eissn=1768-3254&rft_id=info:doi/10.1016/j.ejmech.2022.114946&rft_dat=%3Cproquest_cross%3E2746395787%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=2746395787&rft_id=info:pmid/36459759&rft_els_id=S0223523422008480&rfr_iscdi=true |