{"id":14229,"date":"2024-04-19T07:01:21","date_gmt":"2024-04-19T07:01:21","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=14229"},"modified":"2024-04-19T07:01:21","modified_gmt":"2024-04-19T07:01:21","slug":"2024-discovery-of-a-novel-potent-tetrazole-antifungal-candidate-with-high-selectivity-and-broad-spectrum","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2024-discovery-of-a-novel-potent-tetrazole-antifungal-candidate-with-high-selectivity-and-broad-spectrum\/","title":{"rendered":"2024 &#8211; Discovery of a Novel Potent Tetrazole Antifungal Candidate with High Selectivity and Broad Spectrum"},"content":{"rendered":"<p>Thirty-one novel albaconazole derivatives were designed and synthesized based on our previous work. All compounds exhibited potent\u00a0<i>in vitro<\/i>\u00a0antifungal activities against seven pathogenic fungi. Among them, tetrazole compound\u00a0D2\u00a0was the most potent antifungal with MIC values of &lt;0.008, &lt;0.008, and 2 \u03bcg\/mL against\u00a0<i>Candida albicans<\/i>,\u00a0<i>Cryptococcus neoformans<\/i>, and\u00a0<i>Aspergillus fumigatus<\/i>, respectively, the three most common and critical priority pathogenic fungi. In addition, compound\u00a0D2\u00a0also exhibited potent activity against fluconazole-resistant\u00a0<i>C. auris<\/i>\u00a0isolates. Notably, compound\u00a0D2\u00a0showed a lower inhibitory activity\u00a0<i>in vitro<\/i>\u00a0against human CYP450 enzymes as well as a lower inhibitory effect on the hERG K<sup>+<\/sup>\u00a0channel, indicating a low risk of drug\u2013drug interactions and QT prolongation. Moreover, with improved pharmacokinetic profiles, compound\u00a0D2\u00a0showed better\u00a0<i>in vivo<\/i>\u00a0efficacy than albaconazole at reducing fungal burden and extending the survival of\u00a0<i>C. albicans<\/i>-infected mice. Taken together, compound\u00a0D2\u00a0will be further investigated as a promising candidate.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[53,76],"therapeutic_areas":[143],"target_categories":[61],"target_families":[333],"targets":[92],"resource_keyword":[],"class_list":["post-14229","resource_library","type-resource_library","status-publish","hentry","products_tags-syncropatch-384","resource_type-publication","application_areas-assay-development-and-validation","application_areas-drug-discovery","therapeutic_areas-assay-development-and-validation","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\/14229","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=14229"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=14229"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=14229"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=14229"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=14229"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=14229"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=14229"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=14229"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=14229"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}