Kristiansen J E, Mortensen I
Pharmacol Toxicol. 1987 Feb;60(2):100-3. doi: 10.1111/j.1600-0773.1987.tb01504.x.
Various types of phenothiazines were examined for antibacterial effect on 61 Gram-positive and Gram-negative bacterial strains in vitro. The investigated phenothiazines were two neuroleptic drugs, fluphenazine and chlorpromazine, and two antihistaminic drugs, alimemazine and promethazine. All four drugs have antibacterial effects in vitro, the phenothiazines being more potent against the Gram-positive microorganisms. The antibacterial potency of the drugs was measured as IC50: Fluphenazine 29 microM (15 micrograms/ml), alimemzaine 49 microM (37 micrograms/ml), promethazine 88 microM (28 micrograms/ml) and chlorpromazine 92 microM (29 micrograms/ml). The antibacterial potency of the drugs was linked neither to the neuroleptic nor the antihistaminic potency of the drugs, which is in agreement with results of earlier stereoisomeric investigations. Thus, the known phenothiazines may represent a pool of potentially new antimicrobial drugs. A therapeutic application of these results, however, requires additional in vitro an in vivo testing in an animal model. The bacterial model might be of value as a model system in the study of the interaction of neuropharmacological agents and other membrane active compounds on biological membranes.
研究了多种类型的吩噻嗪类药物对61种革兰氏阳性和革兰氏阴性细菌菌株的体外抗菌作用。所研究的吩噻嗪类药物为两种抗精神病药物氟奋乃静和氯丙嗪，以及两种抗组胺药物阿利马嗪和异丙嗪。所有这四种药物在体外均有抗菌作用，吩噻嗪类药物对革兰氏阳性微生物的作用更强。药物的抗菌效力以IC50衡量：氟奋乃静为29微摩尔（15微克/毫升），阿利马嗪为49微摩尔（37微克/毫升），异丙嗪为88微摩尔（28微克/毫升），氯丙嗪为92微摩尔（29微克/毫升）。药物的抗菌效力与药物的抗精神病效力或抗组胺效力均无关联，这与早期立体异构体研究的结果一致。因此，已知的吩噻嗪类药物可能代表了一个潜在的新型抗菌药物库。然而，要将这些结果应用于治疗，还需要在动物模型中进行额外的体外和体内试验。细菌模型作为研究神经药理学药物和其他膜活性化合物在生物膜上相互作用的模型系统可能具有价值。
