{"id":3773,"date":"2020-08-21T11:21:07","date_gmt":"2020-08-21T09:21:07","guid":{"rendered":"https:\/\/ospt.osi.lv\/?p=3773"},"modified":"2022-01-11T12:16:09","modified_gmt":"2022-01-11T10:16:09","slug":"structure-%e2%80%8bactivity-relationship-studies-on-the-inhibition-of-the-bacterial-translation-of-novel-odilorhabdins-analogues","status":"publish","type":"post","link":"https:\/\/ospt.osi.lv\/structure-%e2%80%8bactivity-relationship-studies-on-the-inhibition-of-the-bacterial-translation-of-novel-odilorhabdins-analogues\/","title":{"rendered":"31. Structure-\u200bactivity relationship studies on the inhibition of the bacterial translation of novel Odilorhabdins analogues"},"content":{"rendered":"<div class=\"wpb-content-wrapper\"><p>[vc_row][vc_column][vc_column_text]Loza, E.; Sarciaux, M.; Ikaunieks, M.; Katkevics, M.; Kukosha, T.; Trufilkina, N.; Ryabova, V.; Shubin, K.; Pantel, L.; Serri, M.; Huseby, D. L.; Cao, S.; Yadav, K.; Hjort, K.; Hughes, D.; Gualtieri, M.; Suna, E.; Racine, E. <em>Bioorg. Med. Chem.<\/em> <strong>2020<\/strong>, <em>28<\/em>, 115469.<\/p>\n<p>DOI: <a title=\"Structure-Activity Relationship Studies on the Inhibition of the Bacterial Translation of Novel Odilorhabdins Analogues\" href=\"https:\/\/doi.org\/10.1016\/j.bmc.2020.115469\" target=\"_blank\" rel=\"nofollow noopener noreferrer\">10.1016\/j.bmc.2020.115469<\/a><\/p>\n<p><!--more--><\/p>\n<h4>Abstract<\/h4>\n<p style=\"text-align: justify;\">A <span class=\"hit\">structure<\/span>-\u200b<span class=\"hit\">activity<\/span> <span class=\"hit\">relationship<\/span> (SAR) study of NOSO-\u200b95179, a nonapeptide from the Odilorhabdin class of antibacterials, was performed by systematic variations of amino acids in positions 2 and 5 of the peptide. \u00a0A series of non-\u200bproteinogenic amino acids was synthesized in high enantiomeric purity from Williams&#8217; chiral diphenyloxazinone by highly diastereoselective alkylation or by Aldol-\u200btype reaction. \u00a0NOSO-\u200b95179 analogs for SAR <span class=\"hit\">studies<\/span> were prepd. using solid-\u200bphase peptide synthesis. \u00a0<span class=\"hit\">Inhibition<\/span> of <span class=\"hit\">bacterial<\/span> <span class=\"hit\">translation<\/span> by each of the synthesized Odilorhabdin analogs was measured using an in vitro test. \u00a0For the most efficient analogs, antibacterial efficacy was measured against two wild-\u200btype Enterobacteriaceae (Escherichia coli and Klebsiella pneumoniae) and against an efflux defective E. coli strain (\u0394tolC) to evaluate the impact of efflux on the antibacterial <span class=\"hit\">activity<\/span>.<\/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]Loza, E.; Sarciaux, M.; Ikaunieks, M.; Katkevics, M.; Kukosha, T.; Trufilkina, N.; Ryabova, V.; Shubin, K.; Pantel, L.; Serri, M.; Huseby, D. L.; Cao, S.; Yadav, K.; Hjort, K.; Hughes, D.; Gualtieri, M.; Suna, E.; Racine, E. Bioorg. Med. Chem. 2020, 28, 115469. DOI: 10.1016\/j.bmc.2020.115469<\/p>\n","protected":false},"author":1,"featured_media":3776,"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\/3773"}],"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\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/comments?post=3773"}],"version-history":[{"count":1,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts\/3773\/revisions"}],"predecessor-version":[{"id":4004,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/posts\/3773\/revisions\/4004"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/media\/3776"}],"wp:attachment":[{"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/media?parent=3773"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/categories?post=3773"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/ospt.osi.lv\/wp-json\/wp\/v2\/tags?post=3773"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}