The fatty acid synthesis inhibitor cerulenin and the structurally unrelated Golgi transport inhibitor brefeldin A are substrates for both types of efflux pumps in Candida albicans. In an effort to overcome efflux pump‐mediated drug resistance in Candida albicans, ceruleninanalogues were generated using a variety of synthesis pathways. The so obtained cerulenin derivatives were tested on multidrug‐resistant