{"id":199,"date":"2024-04-28T22:02:11","date_gmt":"2024-04-28T22:02:11","guid":{"rendered":"https:\/\/src.cikeys.com\/2024\/?page_id=199"},"modified":"2024-04-28T22:42:36","modified_gmt":"2024-04-28T22:42:36","slug":"synthesis-of-conformationally-constrained-di-amino-l-proline-analogues-potential-central-cns-drug-pharmacophores","status":"publish","type":"page","link":"https:\/\/src.cikeys.com\/2024\/conference-schedule\/poster-presentations\/poster-presentations-session-1\/synthesis-of-conformationally-constrained-di-amino-l-proline-analogues-potential-central-cns-drug-pharmacophores\/","title":{"rendered":"Synthesis of Conformationally Constrained di Amino L-Proline Analogues: Potential Central CNS Drug Pharmacophores"},"content":{"rendered":"\n<h2 class=\"wp-block-heading\">Heather Torgerson, &amp; Dr. Thomas Schulze<\/h2>\n\n\n\n<div class=\"wp-block-columns is-layout-flex wp-container-core-columns-is-layout-8f761849 wp-block-columns-is-layout-flex\">\n<div class=\"wp-block-column is-layout-flow wp-block-column-is-layout-flow\" style=\"flex-basis:66.66%\">\n<p class=\"wp-block-paragraph\">Neurosciences (Central Nervous System, CNS) Research &amp; Development (R&amp;D) is a modern field of study with pivotal implications in the pursuit of novel pharmacological studies. Currently available anti-psychotic drugs (aka: Risperidone, Paliperidone) contain 6-Membered Piperidine &amp; Piperazine ring systems which are well-established central pharmacophore systems likely responsible for biological action. Their highly unfavorable side-effect profile is mainly attributed to an enormous amount of Off-Target biological actions, here hypothesized by very high degree of conformational freedoms exerted my 6-Membered Ring Systems. It is hypothesized that conformationally flexible substituted 6-Membered Piperidine ring systems may potentially be responsible for Off-Target biological activity. The research objective is to synthesize conformationally constrained 5- Membered Proline-Based Diamine Analogues. By using Trans-Hydroxy-4-L-Proline as the starting molecule, the diamine analogue is planned to be synthesized in 6 steps. The first 2 synthetic steps have been completed, using small quantities initially and then repeating at larger multi-gram scale. The diamine synthesis is planned to be governed by Lipinski\u2019s Rule-of-Five considerations.<\/p>\n<\/div>\n\n\n\n<div class=\"wp-block-column is-layout-flow wp-block-column-is-layout-flow\" style=\"flex-basis:33.33%\">\n<p class=\"wp-block-paragraph\"><strong><a href=\"https:\/\/src.cikeys.com\/2024\/conference-schedule\/poster-presentations\/\">Poster Presentation<\/a><\/strong><\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><a href=\"https:\/\/src.cikeys.com\/2024\/conference-schedule\/poster-presentations\/poster-presentations-session-1\/\">Session 1<\/a><\/p>\n\n\n\n<p class=\"wp-block-paragraph\">9:15am\u00a0<strong>\u2013<\/strong>\u00a010:30am<br>Grand Salon<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Chemistry<\/strong><\/p>\n<\/div>\n<\/div>\n","protected":false},"excerpt":{"rendered":"<p>Heather Torgerson, &amp; Dr. Thomas Schulze Neurosciences (Central Nervous System, CNS) Research &amp; Development (R&amp;D) is a modern field of study with pivotal implications in the pursuit of novel pharmacological studies. Currently available anti-psychotic drugs (aka: Risperidone, Paliperidone) contain 6-Membered Piperidine &amp; Piperazine ring systems which are well-established central pharmacophore systems likely responsible for biological [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"parent":45,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"footnotes":""},"categories":[5,6],"tags":[29],"class_list":["post-199","page","type-page","status-publish","hentry","category-poster-presentations","category-session-1","tag-chemistry","post"],"_links":{"self":[{"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/pages\/199","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/comments?post=199"}],"version-history":[{"count":2,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/pages\/199\/revisions"}],"predecessor-version":[{"id":394,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/pages\/199\/revisions\/394"}],"up":[{"embeddable":true,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/pages\/45"}],"wp:attachment":[{"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/media?parent=199"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/categories?post=199"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/src.cikeys.com\/2024\/wp-json\/wp\/v2\/tags?post=199"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}