{"id":13341,"date":"2023-11-17T16:37:40","date_gmt":"2023-11-17T16:37:40","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=13341"},"modified":"2024-01-10T16:38:04","modified_gmt":"2024-01-10T16:38:04","slug":"2023-discovery-of-novel-8-hydroxyquinoline-derivatives-with-potent-in-vitro-and-in-vivo-antifungal-activity","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2023-discovery-of-novel-8-hydroxyquinoline-derivatives-with-potent-in-vitro-and-in-vivo-antifungal-activity\/","title":{"rendered":"2023 &#8211; Discovery of Novel 8-Hydroxyquinoline Derivatives with Potent In Vitro and In Vivo Antifungal Activity"},"content":{"rendered":"<p>Fungal pathogens can cause life-threatening infections, yet current antifungals are inadequate at treating many of these, highlighting the importance of novel drug discovery. Here, we report hit compound\u00a0<b>L14<\/b>, a novel 8-hydroxyquinoline derivative with potent and broad-spectrum antifungal activity.\u00a0<i>In vitro<\/i>\u00a0experiments exhibited that\u00a0<b>L14<\/b>\u00a0had better activity and lower cytotoxicity than that of clioquinol and showed synergy in combination with fluconazole (FLC). In a\u00a0<i>Candida albicans<\/i>-infected murine model,\u00a0<b>L14<\/b>\u00a0at 2 mg\/kg showed better\u00a0<i>in vivo<\/i>\u00a0efficacy than clioquinol at reducing fungal burden and extending the survival of\u00a0<i>C. albicans<\/i>-infected mice. In addition,\u00a0<b>L14<\/b>\u00a0alone or in combination with FLC had significant inhibitory activity against hypha and biofilm formation. Overall, our data indicated that 8-hydroxyquinoline derivative\u00a0<b>L14<\/b>\u00a0has favorable pharmacokinetics and acceptable safety profiles and could be further investigated as a promising antifungal hit compound.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[50,76],"therapeutic_areas":[54],"target_categories":[61],"target_families":[333],"targets":[92],"resource_keyword":[],"class_list":["post-13341","resource_library","type-resource_library","status-publish","hentry","products_tags-syncropatch-384","resource_type-publication","application_areas-ion-channels","application_areas-drug-discovery","therapeutic_areas-cardiac-safety-cipa","target_categories-voltage-gated-ion-channels","target_families-kv-channels","targets-kv11-1-herg"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/13341","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library"}],"about":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/types\/resource_library"}],"wp:attachment":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/media?parent=13341"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=13341"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=13341"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=13341"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=13341"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=13341"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=13341"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=13341"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=13341"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}