Ecocompatible Asymmetric Catalysis Laboratory (LCAE) Badji Mokhtar Annaba-University, B.P 12, 23000 Annaba, Algeria.
Ecocompatible Asymmetric Catalysis Laboratory (LCAE) Badji Mokhtar Annaba-University, B.P 12, 23000 Annaba, Algeria.
Bioorg Med Chem Lett. 2021 Jun 1;41:128000. doi: 10.1016/j.bmcl.2021.128000. Epub 2021 Mar 30.
(S, S)-1-hydroxy-1-oxo-2-c,5-t-diphenylphospholane or Fiaud's acid is used as a novel and effective chiral organocatalyst for bis α-aminophosphonates synthesis with excellent diastereoselectivity and yields within short reaction time. All synthesized bis α-aminophosphonates revealed a good to excellent antifungal capacity, where the six compounds 4a, 4b, 4e, 4h, 4k and 4l are the best fungicide inhibiting the growth of Fusarium oxysporumandBotrytis cinereaby 65% to 84% with IC values <0.02 mg/mL. Similarly, these six products exhibited a strong antioxidant effect, whereas a low inhibition activity was obtained with both AChE and BChE. Furthermore, they displayed a very weak inhibitory activity against tyrosinase except for the compound4l.These findings suggest a possible use of these compounds as synthetic pesticides with less hazardous effects with antioxidant, and anti-tyrosinase properties.
（S，S）-1-羟基-1-氧代-2-C，5-t-二苯基膦杂环戊烷或 Fiaud 酸被用作一种新型有效的手性有机催化剂，用于双 α-氨基膦酸酯的合成，具有出色的非对映选择性和较短反应时间内的产率。所有合成的双 α-氨基膦酸酯都表现出良好到优异的抗真菌能力，其中 6 种化合物 4a、4b、4e、4h、4k 和 4l 是最好的杀菌剂，对尖孢镰刀菌和灰葡萄孢的生长抑制率为 65%至 84%，IC 值 <0.02 mg/mL。同样，这 6 种产品表现出很强的抗氧化作用，而 AChE 和 BChE 的抑制活性很低。此外，它们对酪氨酸酶的抑制活性很弱，除了化合物 4l 之外。这些发现表明，这些化合物可能被用作具有抗氧化和抗酪氨酸酶特性的低危害性合成农药。
