Departamento de Química Orgánica, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez, 2, 38206 La Laguna, Tenerife, Spain.
Centro Atlántico del Medicamento S.A. (CEAMED S.A.), PCTT, 38200 La Laguna, Tenerife, Spain.
Molecules. 2024 Oct 11;29(20):4811. doi: 10.3390/molecules29204811.
Pharmaceutical and veterinary products are a class of contaminants of emerging concern, and their presence in the environment is due to continuous and incorrect disposal. Environmental scientists have been accumulating data on their adverse effects on animal populations since toxicological effects on wildlife were first published. Therefore, recycling strategies are needed. Valuable active ingredients can be extracted from expired pharmaceuticals and recycled according to various strategies. In an effort to reveal the potential of the chemical upcycling of expired pharmaceuticals, the active ingredients gabapentin and pregabalin were extracted and used as starting materials to prepare a small collection of promising substrates endowed with functionalities and structural three-dimensionality. Gabapentin was transformed into aminoalcohol , spiroamine and the bioactive azaspirolactam . The lactam analog was synthesized from pregabalin . Due to the biological profile of and the structural similarity of the -alkylated derivatives and with the drug piracetam, a collection of potentially bioactive structural analogs and were also prepared. Simple extraction, synthesis, and purification procedures were used as a means of chemical and economic revaluation, resulting in moderate to good yields at a low cost.
药品和兽药是一类新兴关注的污染物,它们在环境中的存在是由于持续和不正确的处理。环境科学家一直在积累有关它们对动物种群的不良影响的数据,因为首次发表了关于野生动物的毒理学影响。因此,需要回收策略。可以从过期药品中提取有价值的活性成分,并根据各种策略进行回收。为了揭示化学升级改造过期药品的潜力,从过期药品中提取了活性成分加巴喷丁和普瑞巴林,并将其用作起始原料,制备了一系列具有功能和结构三维性的有前途的底物。将加巴喷丁转化为氨基醇、螺环胺和生物活性氮杂螺环内酰胺。从普瑞巴林合成了内酰胺类似物。由于 和 的生物特征以及 - 烷基化衍生物 和 与药物吡拉西坦的结构相似性,还制备了一系列潜在的生物活性结构类似物 和 。简单的提取、合成和纯化程序被用作化学和经济再评估的手段,以低成本获得中等至良好的收率。