Carcelli M, Mazza P, Pelizzi C, Pelizzi G, Zani F
Istituto di Chimica Generale ed Inorganica, Università di Parma, Italy.
J Inorg Biochem. 1995 Jan;57(1):43-62. doi: 10.1016/0162-0134(94)00004-t.
The antibacterial and antifungal properties of five 2,6-diacetylpyridine bis(acylhydrazones) (acyl:benzoyl, H2dapb; 2-aminobenzoyl, H2dapab; salicyloyl, H2daps; picolinoyl, H2dappc; 2-thenoyl, H2dapt) and of a series of metal complexes were investigated. The x-ray crystal structure of the [Cu(dapt)]2 complex was also determined. It consists of dimeric units in which both copper atoms have sixfold coordination. The evaluation of in vitro antimicrobial properties showed some compounds to exhibit good activity against Gram positive bacteria. In most cases, complexes showed a similar or reduced activity as compared to the ligand itself. Only the iron complexes were found to be more active than the chelating agent involved. None of the compounds showed any significant antifungal activity. The genotoxicity of the compounds described was studied in vitro with Bacillus subtilis rec-assay and Salmonella-microsome reversion assay. No DNA-damaging activity was detected in the Bacillus subtilis rec-assay. H2dapb, H2dapb, and H2dappc were active in the Salmonella test. In several cases, the genotoxic properties of the ligands disappeared in the complexes.
研究了五种2,6 - 二乙酰基吡啶双(酰腙)(酰基:苯甲酰基,H2dapb;2 - 氨基苯甲酰基,H2dapab;水杨酰基,H2daps;吡啶甲酰基,H2dappc;2 - 噻吩甲酰基,H2dapt)以及一系列金属配合物的抗菌和抗真菌性能。还测定了[Cu(dapt)]2配合物的X射线晶体结构。它由二聚体单元组成,其中两个铜原子都具有六配位。体外抗菌性能评估表明,一些化合物对革兰氏阳性菌表现出良好的活性。在大多数情况下,配合物与配体本身相比表现出相似或降低的活性。仅发现铁配合物比所涉及的螯合剂更具活性。没有一种化合物表现出任何显著的抗真菌活性。用枯草芽孢杆菌rec - 试验和沙门氏菌 - 微粒体回复试验在体外研究了所述化合物的遗传毒性。在枯草芽孢杆菌rec - 试验中未检测到DNA损伤活性。H2dapb、H2dapb和H2dappc在沙门氏菌试验中具有活性。在几种情况下,配体的遗传毒性特性在配合物中消失。