Dymicky M, Huhtanen C N, Wasserman A E
Antimicrob Agents Chemother. 1977 Sep;12(3):353-6. doi: 10.1128/AAC.12.3.353.
A number of 5-nitrothiazoles with various substituents in the 2-position were tested for inhibition of Clostridium botulinum in a culture medium. Thiazole itself or 2-bromo- or 2-methylthiazole at 30 mug/ml did not inhibit the organism. An amino group in the 2-position of thiazole inhibited at 10 mug/ml. Substitution of a nitro group in the 5-position of 2-aminothiazole increased the inhibitory level to 0.12 mug/ml; acetyl-, propionyl-, or butyroyl-2-amino-5-nitrothiazole inhibited at 0.04 mug/ml. Benzoyl-2-amino-5-nitrothiazole inhibited at 0.16 mug/ml; this increased to 0.01 mug/ml when the benzoyl group carried a nitro group in the m- or p-position; a nitro group in the o-position, on the other hand, inhibited at 0.04 mug/ml. Unsaturated aliphatic acyls decreased inhibition. The greatest activity was exhibited by 2-nonanoyl- and 2-lauroylamides, with minimum inhibitory concentrations of 0.005 and 0.0025 mug/ml, respectively.
测试了一些在2-位带有各种取代基的5-硝基噻唑对培养基中肉毒梭菌的抑制作用。噻唑本身或30μg/ml的2-溴噻唑或2-甲基噻唑均不抑制该菌。噻唑2-位上的氨基在10μg/ml时具有抑制作用。2-氨基噻唑5-位上取代一个硝基可使抑制水平提高到0.12μg/ml；乙酰基-、丙酰基-或丁酰基-2-氨基-5-硝基噻唑在0.04μg/ml时具有抑制作用。苯甲酰基-2-氨基-5-硝基噻唑在0.16μg/ml时具有抑制作用；当苯甲酰基在间位或对位带有一个硝基时，抑制作用增强到0.01μg/ml；而邻位带有硝基时，抑制作用为0.04μg/ml。不饱和脂肪酰基会降低抑制作用。2-壬酰基和2-月桂酰基酰胺表现出最大活性，最低抑菌浓度分别为0.005和0.0025μg/ml。
