Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.
Postgraduate Program in Bioscience & Physiopathology, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.
Future Microbiol. 2019 Jul;14:981-994. doi: 10.2217/fmb-2019-0040. Epub 2019 Aug 6.
To evaluate the potential of three benzohydrazones (-), four acylhydrazones derived from isoniazid (INH-acylhydrazones) (-) and one hydrazone () as antituberculosis agents. Inhibitory and bactericidal activities were determined for the reference () strain and clinical isolates. Cytotoxicity, drug combinations and ethidium bromide accumulation assays were also performed. The tested compounds (-) presented excellent antituberculosis activity with surprisingly inhibitory (0.12-250 μg/ml) and bactericidal values, even against multidrug-resistant clinical isolates. Compounds showed high selectivity index, with values reaching 1833.33, and a limited spectrum of activity. Some of the compounds ( & ) are also great inhibitors of bacillus efflux pumps. Benzohydrazones and INH-acylhydrazones may be considered scaffolds for the development of new anti- drugs.
为了评估三种苯腙（-）、四种异烟酰腙（INH-酰腙）（-）和一种腙（）作为抗结核药物的潜力。对参考（）株和临床分离株进行了抑制和杀菌活性的测定。还进行了细胞毒性、药物组合和溴化乙锭积累测定。 测试化合物（-）表现出优异的抗结核活性，令人惊讶的是具有抑制（0.12-250μg/ml）和杀菌作用，甚至对耐多药临床分离株也有作用。化合物具有高选择性指数，值可达 1833.33，且活性范围有限。一些化合物（&）也是芽孢杆菌外排泵的有效抑制剂。 苯腙和 INH-酰腙可能被认为是开发新型抗结核药物的支架。
