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新型 Ga(III) 多吡啶儿茶酚配合物的合成、表征及抗菌活性。

Synthesis, characterisation and antibacterial activity of novel Ga(III) polypyridyl catecholate complexes.

机构信息

School of Food Science & Environmental Health, Technological University Dublin, Dublin 7, Ireland.

SSPC, the Science Foundation Ireland Research Centre for Pharmaceuticals, Ireland.

出版信息

Dalton Trans. 2023 Aug 29;52(34):11958-11964. doi: 10.1039/d3dt01761c.

Abstract

Ga(III) polypyridyl catecholate complexes of type Ga(bipy)(O,O) or Ga(phen)(O,O) respectively were readily synthesised on reaction of Ga(NO) in methanol with 1 equivalent of catecholate ligand (2,3-DHBA, 3,4-DHBA, 2,3,4-THBA or CafA) and then 2 equivalents of either bipy or phen. The complexes were characterised in full including by X-ray crystallography, which established that the catecholate ligands coordinate the Ga(III) centres in a bidentate manner the two deprotonated hydroxy groups. All Ga(III) complexes exhibited good antibacterial activity against the Gram-negative pathogenic bacteria , and . The complexes were inactive against the Gram-positive pathogenic bacteria including against a methicillin-resistant strain (MRSA). Ga(bipy)(2,3-DHBA)·1.5HO (1) was shown to be non toxic in larvae of at doses up to 2000 μg mL and to offer protection at doses of 100 and 250 μg mL at 48 and 96 h to larvae infected with .

摘要

Ga(III) 多酚儿茶酚配合物类型Ga(bipy)(O,O)Ga(phen)(O,O)分别通过 Ga(NO)在甲醇中的反应容易合成,反应中使用 1 当量儿茶酚配体(2,3-DHBA、3,4-DHBA、2,3,4-THBA 或 CafA),然后使用 2 当量的 bipy 或 phen。该配合物被全面表征,包括通过 X 射线晶体学,其确定儿茶酚配体以双齿配位方式将 Ga(III)中心配位,其中两个去质子化的羟基团。所有 Ga(III)配合物都表现出对革兰氏阴性病原菌的良好抗菌活性,包括对革兰氏阳性病原菌无效,包括对耐甲氧西林的金黄色葡萄球菌 (MRSA) 菌株。Ga(bipy)(2,3-DHBA)·1.5HO(1)在高达 2000μg/mL 的剂量下在幼虫中显示出非毒性,并且在 48 和 96 h 时在 100 和 250μg/mL 的剂量下为感染的幼虫提供保护。

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