Zakula D, Capobianco J O, Goldman R C
Anti-infective Research Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
J Antimicrob Chemother. 1997 Feb;39(2):261-4. doi: 10.1093/jac/39.2.261.
We have identified four non-azole inhibitors of lanosterol 14a-demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC50 values for ergosterol inhibition of 0.9 microM (0.3 mg/L) and 1.9 microM (0.6 mg/L) in whole cell and cell-free extract assays, respectively. A-39806 demonstrated broad in-vitro antifungal activity against several Candida species as well as against Cryptococcus albidus and Aspergillus niger. In-vitro antifungal activity was also demonstrated against a fluconazole-resistant clinical isolate of C. albicans.
我们已经在白色念珠菌CCH442中鉴定出四种羊毛甾醇14α-脱甲基酶的非唑类抑制剂。最有效的化合物A-39806在全细胞和无细胞提取物试验中对麦角甾醇抑制的IC50值分别为0.9微摩尔（0.3毫克/升）和1.9微摩尔（0.6毫克/升）。A-39806对几种念珠菌属物种以及白色隐球菌和黑曲霉表现出广泛的体外抗真菌活性。对白色念珠菌的氟康唑耐药临床分离株也表现出体外抗真菌活性。
