Gurkok Gokce, Altanlar Nurten, Suzen Sibel
Department of Pharmaceutical Chemistry, Ankara University, Faculty of Pharmacy, Tandogan, Ankara, Turkey.
Chemotherapy. 2009;55(1):15-9. doi: 10.1159/000166999. Epub 2008 Oct 31.
Indoles and hydrazone-type compounds constitute an important class of compounds for new drug development in order to discover an effective compound against multi-drug-resistant microbial infections.
A series of indole-3-aldehyde and 5-bromoindole-3-aldehyde hydrazide and hydrazones was evaluated for their in vitro antimicrobial activities using the 2-fold serial dilution technique against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Escherichia coli, Bacillus subtilis and Candida albicans. The minimum inhibitory concentration (MIC) was determined for test compounds and for the reference standards sultamicillin, ampicillin, fluconazole and ciprofloxacin.
Compounds possessed a broad spectrum of activity having MIC values of 6.25-100 mg/ml against the tested microorganisms. Compounds 1a-1j, in particular, displayed better activity against MSRA and significant activity against S. aureus relative to ampicillin. Unexpectedly, indole nicotinic acid hydrazides showed no significant activity while indole anisic acid hydrazides displayed better activity.
The results may be instructive to researchers attempting to gain more understanding of the antimicrobial activity of indole hydrazide/hydrazone-type compounds.
吲哚和腙类化合物是新药开发中的一类重要化合物，旨在发现一种有效的抗多重耐药微生物感染的化合物。
采用两倍系列稀释技术，对一系列吲哚 - 3 - 醛、5 - 溴吲哚 - 3 - 醛酰肼和腙对金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌（MRSA）、大肠杆菌、枯草芽孢杆菌和白色念珠菌的体外抗菌活性进行了评估。测定了受试化合物以及参考标准药物舒他西林、氨苄西林、氟康唑和环丙沙星的最低抑菌浓度（MIC）。
化合物具有广谱活性，对受试微生物的MIC值为6.25 - 100 mg/ml。特别是化合物1a - 1j，相对于氨苄西林，对MRSA表现出更好的活性，对金黄色葡萄球菌表现出显著活性。出乎意料的是，吲哚烟酸酰肼没有显著活性，而吲哚茴香酸酰肼表现出更好的活性。
这些结果可能对试图更深入了解吲哚酰肼/腙类化合物抗菌活性的研究人员具有指导意义。
