Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties

Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties | Research Square window.SnipcartSettings = { analytics: { enabled: false } }; (function() { var accessVector = localStorage.getItem('access_vector') || ''; window.dataLayer = window.dataLayer || []; if (accessVector) { window.dataLayer.push({ user: { profile: { profileInfo: { snid: accessVector } } } }); } })(); (function(w,d,s,l,i){w[l]=w[l]||[];w[l].push({'gtm.start':new Date().getTime(),event:'gtm.js'});var f=d.getElementsByTagName(s)[0],j=d.createElement(s),dl=l!='dataLayer'?'&l='+l:'';j.async=true;j.src='https://www.googletagmanager.com/gtm.js?id='+i+dl;f.parentNode.insertBefore(j,f);})(window,document,'script','dataLayer','GTM-K279D39R'); Browse Preprints In Review Journals COVID-19 Preprints AJE Video Bytes Research Tools Research Promotion AJE Professional Editing AJE Rubriq About Preprint Platform In Review Editorial Policies Our Team Advisory Board Help Center Sign In Submit a Preprint Cite Share Download PDF Research Article Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties Ronewa Tshinavhe, Nashied Peton, Sandile B. Simelane, Paseka Moshapo This is a preprint; it has not been peer reviewed by a journal. https://doi.org/ 10.21203/rs.3.rs-4705905/v1 This work is licensed under a CC BY 4.0 License Status: Published Journal Publication published 18 Oct, 2024 Read the published version in Medicinal Chemistry Research → Version 1 posted 5 You are reading this latest preprint version Abstract Tuberculosis (TB) continues to be a threat to global health stability. Pyrimidine carboxamides have demonstrated potent anti-tubercular properties against clinical Mycobacterium tuberculosis , the causative agent of TB. Herein, we report a follow-up study on the synthesis of pyrimidine carboxamide molecular analogues and their anti-TB evaluation. In total, a library consisting of 37 new compounds is reported. Seven compounds ( 7b , 7d , 7m , 7p , 7q , 7aa , and 7ah ) demonstrated excellent in vitro activities with MIC 90 values below 1.00 µM. Apart from compound 7ah , compounds with improved aqueous solubility properties had lower anti-TB potency. Preliminary mode of action studies using bioluminescence assays indicate that the active compounds do not affect the integrity of mycobacterial DNA or the cell wall. The active compounds were also found to be bactericidal against replicating H37Rv Mtb strain. Full Text Supplementary Files SupportingInformationMedChemRes.pdf Cite Share Download PDF Status: Published Journal Publication published 18 Oct, 2024 Read the published version in Medicinal Chemistry Research → Version 1 posted Editorial decision: Major Revision 29 Aug, 2024 Reviewers agreed at journal 15 Jul, 2024 Reviewers invited by journal 15 Jul, 2024 Editor assigned by journal 12 Jul, 2024 First submitted to journal 09 Jul, 2024 You are reading this latest preprint version Research Square lets you share your work early, gain feedback from the community, and start making changes to your manuscript prior to peer review in a journal. As a division of Research Square Company, we’re committed to making research communication faster, fairer, and more useful. We do this by developing innovative software and high quality services for the global research community. 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Also discoverable on Platform About Our Team In Review Editorial Policies Advisory Board Help Center Resources Author Services Accessibility API Access RSS feed Manage Cookie Preferences © Research Square 2026 | ISSN 2693-5015 (online) Privacy Policy Terms of Service Do Not Sell My Personal Information {"props":{"pageProps":{"initialData":{"identity":"rs-4705905","acceptedTermsAndConditions":true,"allowDirectSubmit":false,"archivedVersions":[],"articleType":"Research Article","associatedPublications":[],"authors":[{"id":327278225,"identity":"3002c91f-6838-4a7a-9f52-405df47b2bb4","order_by":0,"name":"Ronewa Tshinavhe","email":"","orcid":"","institution":"University of Johannesburg","correspondingAuthor":false,"prefix":"","firstName":"Ronewa","middleName":"","lastName":"Tshinavhe","suffix":""},{"id":327278226,"identity":"a252e80b-afec-4458-a26d-3399e1410c47","order_by":1,"name":"Nashied Peton","email":"","orcid":"","institution":"University of Cape Town","correspondingAuthor":false,"prefix":"","firstName":"Nashied","middleName":"","lastName":"Peton","suffix":""},{"id":327278227,"identity":"8972868e-c721-4e60-998f-28ab3cc89b74","order_by":2,"name":"Sandile B. 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