Bis(N-picolinamido)cobalt(II) Complexes Display Antifungal Activity toward Candida albicans and Aspergillus fumigatus.

Bis(N-picolinamido)cobalt(II) Complexes Display Antifungal Activity toward Candida albicans and Aspergillus fumigatus.
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DOI:
10.1002/cmdc.202100159
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发表时间:
2021-10-15
期刊:
影响因子:
3.4
通讯作者:
McGowan PC
McGowan PC
中科院分区:
医学4区
文献类型:
--
作者:
Ghandhi LHD;Bidula S;Pask CM;Lord RM;McGowan PC

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本文报道了十个新的[(L)2CoX2]0/2+型双(N-吡啶甲酰胺基)钴(II)配合物的合成和表征,其中L=N-吡啶甲酰胺配体,X=二异硫氰酸根(−ncs)、二氯(−Cl)或二水(−OH2)配体。对其中9个结构进行了单晶X-射线衍射分析,证实吡啶甲酰胺以中性N,O键的方式与Co(II)中心结合。通过粉末X-射线衍射仪的分析,确定了各配合物的顺式和反式配位。所有的化合物都对几种真菌进行了筛选,并显示出更强的抗真菌活性。值得注意的是,这些化合物对白色念珠菌和烟曲霉有显著的抑制活性,其中几个化合物对~gt;80 %的生长有抑制作用,一个化合物对烟曲霉的菌丝生长抑制>90 %。相反,对新生隐球菌无抗真菌活性,对哺乳动物细胞系无细胞毒性。据报道,与顺式配合物相比,含有反式异硫氰酸酯配体的双(N-吡啶甲酰胺)钴(II)配合物对真菌的活性显著增强。它们对真菌菌株的生长抑制率为80 %,对细菌或哺乳动物细胞没有毒性报道。
This report highlights the synthesis and characterization of ten new bis(N‐picolinamido)cobalt(II) complexes of the type [(L)2CoX2]0/2+, whereby L=N‐picolinamide ligand and X=diisothiocyanato (−NCS), dichlorido (−Cl) or diaqua (−OH2) ligands. Single crystal X‐ray (SC‐XRD) analysis for nine of the structures are reported and confirm the picolinamide ligand is bound to the Co(II) center through a neutral N,O binding mode. With the addition of powder X‐ray diffraction (PXRD), we have confirmed the cis and trans ligand arrangements of each complex. All complexes were screened against several fungal species and show increased antifungal activity. Notably, these complexes had significant activity against strains of Candida albicans and Aspergillus fumigatus, with several compounds exhibiting growth inhibition of >80 %, and onecompound inhibiting Aspergillus fumigatus hyphal growth by >90 %. Conversely, no antifungal activity was exhibited toward Cryptococcus neoformans and no cytotoxicity towards mammalian cell lines. Bis(N‐picolinamide)cobalt(II) complexes containing trans isothiocyanate ligands are reported to have significantly enhanced activity toward fungal species, when compared the cis complexes. They display >80 % growth inhibition of fungal strains and no reported toxicity toward bacterial species or mammalian cells.
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