{"id":4239,"date":"2023-10-17T18:27:03","date_gmt":"2023-10-17T16:27:03","guid":{"rendered":"https:\/\/ospt.osi.lv\/?p=4239"},"modified":"2023-10-17T19:38:08","modified_gmt":"2023-10-17T17:38:08","slug":"synthesis-and-evaluation-of-novel-5-o-4-c-aminoalkyl-%ce%b2-d-ribofuranosyl-apramycin-derivatives-for-the-inhibition-of-gram-negative-pathogens-carrying-the-aminoglycoside-phosphotransferase3","status":"publish","type":"post","link":"https:\/\/ospt.osi.lv\/synthesis-and-evaluation-of-novel-5-o-4-c-aminoalkyl-%ce%b2-d-ribofuranosyl-apramycin-derivatives-for-the-inhibition-of-gram-negative-pathogens-carrying-the-aminoglycoside-phosphotransferase3\/","title":{"rendered":"49. Synthesis and Evaluation of Novel 5-O-(4-C-Aminoalkyl-\u03b2-D-ribofuranosyl) Apramycin Derivatives for the Inhibition of Gram-Negative Pathogens Carrying the Aminoglycoside Phosphotransferase(3\u2032)-Ia Resistance Determinant"},"content":{"rendered":"<div class=\"wpb-content-wrapper\"><p>[vc_row][vc_column][vc_column_text]Lubriks, D.; Haldimann, K.; Kili\u00e7, F.; Hartmann, M.; B\u00f6ttger, E. C.; Hobbie, S. N.; Suna, E.; Crich, D. <em>Helv. Chim. Acta<span dir=\"ltr\">\u00a0<\/span><\/em><strong><span dir=\"ltr\">2023<\/span><\/strong><span dir=\"ltr\">, e202300138<\/span><br \/>\nDOI: <a title=\"Synthesis and Evaluation of Novel 5-O-(4-C-Aminoalkyl-\u03b2-D-ribofuranosyl) Apramycin Derivatives for the Inhibition of Gram-Negative Pathogens Carrying the Aminoglycoside Phosphotransferase(3\u2032)-Ia Resistance Determinant\" href=\"http:\/\/10.1002\/hlca.202300138\" target=\"_blank\" rel=\"nofollow noopener\">10.1002\/hlca.202300138<\/a>.<\/p>\n<p>&nbsp;<\/p>\n<p><!--more--><\/p>\n<h4>Abstract<\/h4>\n<p style=\"text-align: justify;\">We report the synthesis and evaluation of two new apramycin 5-O-\u03b2-d-ribofuranosides, or apralogs, carrying aminoalkyl branches at the ribofuranose 4-position. This novel modification conveys excellent activity for the inhibition of protein synthesis by wild-type bacterial ribosomes and correspondingly high antibacterial activity against several Gram-negative pathogens. Notably, these new modifications overcome the reduction of antibacterial activity in other 2-deoxystreptamine-type aminoglycosides carrying a 5-O-ribofuranosyl moiety when challenged by the presence of an aminoglycoside phosphotransferase enzyme capable of acting on the ribose 5-position.<\/p>\n<p>[\/vc_column_text][\/vc_column][\/vc_row]<\/p>\n<\/div>","protected":false},"excerpt":{"rendered":"<p>[vc_row][vc_column][vc_column_text]Lubriks, D.; Haldimann, K.; Kili\u00e7, F.; Hartmann, M.; B\u00f6ttger, E. C.; Hobbie, S. N.; Suna, E.; Crich, D. Helv. Chim. Acta\u00a02023, e202300138 DOI: 10.1002\/hlca.202300138. &nbsp;<\/p>\n","protected":false},"author":5,"featured_media":4244,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"image","meta":{"_exactmetrics_skip_tracking":false,"_exactmetrics_sitenote_active":false,"_exactmetrics_sitenote_note":"","_exactmetrics_sitenote_category":0,"footnotes":""},"categories":[40,16],"tags":[],"aioseo_notices":[],"_links":{"self":[{"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts\/4239"}],"collection":[{"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/users\/5"}],"replies":[{"embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/comments?post=4239"}],"version-history":[{"count":2,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts\/4239\/revisions"}],"predecessor-version":[{"id":4241,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts\/4239\/revisions\/4241"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/media\/4244"}],"wp:attachment":[{"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/media?parent=4239"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/categories?post=4239"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/tags?post=4239"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}