{"id":6608,"date":"2023-02-17T07:14:53","date_gmt":"2023-02-17T07:14:53","guid":{"rendered":"https:\/\/beta.nanion.de\/resource_library\/2022-discovery-of-novel-7-hydroxy-5-oxo-45-dihydrothieno32-bpyridine-6-carboxamide-derivatives-with-potent-and-selective-antifungal-activity-against-cryptococcus-species\/"},"modified":"2023-02-17T07:14:54","modified_gmt":"2023-02-17T07:14:54","slug":"2022-discovery-of-novel-7-hydroxy-5-oxo-45-dihydrothieno32-bpyridine-6-carboxamide-derivatives-with-potent-and-selective-antifungal-activity-against-cryptococcus-species","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2022-discovery-of-novel-7-hydroxy-5-oxo-45-dihydrothieno32-bpyridine-6-carboxamide-derivatives-with-potent-and-selective-antifungal-activity-against-cryptococcus-species\/","title":{"rendered":"2022 &#8211; Discovery of Novel 7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-b]pyridine-6-carboxamide Derivatives with Potent and Selective Antifungal Activity against Cryptococcus Species"},"content":{"rendered":"<p>Cryptococcus neoformans\u00a0and\u00a0Cryptococcus gattii\u00a0can cause fatal invasive infections, especially in immunocompromised patients. However, few antifungal drugs are available to help treat cryptococcosis. In this study, by compound library screening, we presented the first report of hit compound\u00a0P163-0892, which had potent\u00a0in vitro\u00a0and\u00a0in vivo\u00a0antifungal activity against\u00a0Cryptococcus\u00a0spp.\u00a0In vitro\u00a0tests showed that\u00a0P163-0892\u00a0was not cytotoxic and had highly selective and strong antifungal activities against\u00a0Cryptococcus\u00a0spp. with MIC values less than 1 \u03bcg\/mL. Synergism of\u00a0P163-0892\u00a0and fluconazole was also observed\u00a0in vitro. The\u00a0in vivo\u00a0antifungal efficacy of\u00a0P163-0892\u00a0was assessed in a wax moth larval fungal infection model, and treatment with 10 mg\/kg\u00a0P163-0892\u00a0caused a significant reduction in fungal burden and significant extension of the survival time. Taken together, our data indicate that the hit compound\u00a0P163-0892\u00a0warrants further investigation as a novel anti-Cryptococcus\u00a0agent.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[50,76],"therapeutic_areas":[],"target_categories":[],"target_families":[],"targets":[],"resource_keyword":[],"class_list":["post-6608","resource_library","type-resource_library","status-publish","hentry","products_tags-syncropatch-384","resource_type-publication","application_areas-ion-channels","application_areas-drug-discovery"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/6608","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=6608"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=6608"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=6608"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=6608"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=6608"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=6608"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=6608"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=6608"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=6608"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}