Mood Aaron D, Premachandra Ilandari Dewage Udara Anulal, Hiew Stanley, Wang Fuqiang, Scott Kevin A, Oldenhuis Nathan J, Liu Haoping, Van Vranken David L
Department of Chemistry, University of California , 1102 Natural Sciences 2, Irvine, California 92697-2025, United States.
Department of Biological Chemistry, University of California , Irvine, California 92697-1700, United States.
ACS Med Chem Lett. 2017 Jan 11;8(2):168-173. doi: 10.1021/acsmedchemlett.6b00355. eCollection 2017 Feb 9.
Four phthalazinones (CIDs 22334057, 22333974, 22334032, 22334012) and one isoquinolone (CID 5224943) were previously shown to be potent enhancers of antifungal activity of fluconazole against . Several even more potent analogues of these compounds were identified, some with EC as low as 1 nM, against . The compounds exhibited pharmacological synergy (FIC < 0.5) with fluconazole. The compounds were also shown to enhance the antifungal activity of isavuconazole, a recently FDA approved azole antifungal. Isoquinolone and phthalazinone were shown to be active against several resistant clinical isolates of .
四种酞嗪酮（化合物识别号22334057、22333974、22334032、22334012）和一种异喹诺酮（化合物识别号5224943）先前已被证明是氟康唑抗……抗真菌活性的强效增强剂。针对……鉴定出了这些化合物的几种活性更强的类似物，有些化合物的最低半数效应浓度（EC）低至1纳摩尔。这些化合物与氟康唑表现出药理学协同作用（联合药敏系数<0.5）。这些化合物还被证明可增强艾沙康唑（一种最近获美国食品药品监督管理局批准的唑类抗真菌药）的抗真菌活性。异喹诺酮和酞嗪酮对几种……耐药临床分离株具有活性。
