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铋化合物在药物化学中的应用。

Bismuth compounds in medicinal chemistry.

机构信息

Laboratório de Química Farmacêutica, Faculdade de Farmácia da Universidade de Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, Coimbra, Portugal.

出版信息

Future Med Chem. 2012 Jul;4(11):1495-523. doi: 10.4155/fmc.12.95.

Abstract

In recent years, the chemical potential of bismuth and bismuth compounds has been actively exploited. Bismuth salts are known for their low toxicity, making them potential valuable reagents for large-scale synthesis, which becomes more obvious when dealing with products such as active pharmaceutical ingredients or synthetic intermediates. Conversely, bismuth compounds have been widely used in medicine. After extensive use in the treatments of syphilis and other bacterial infections before the advent of modern antibiotics, bismuth compounds remain important for the treatment of several gastrointestinal disorders and also exhibit antimicrobial properties and cytotoxic activity, among others. This review updates relevant advances in the past few years, concerning the application of bismuth reagents and catalysts in innovative synthetic processes for the preparation of compounds of medicinal interest, as well as the preparation, biological evaluation and potential medicinal uses of bismuth compounds.

摘要

近年来,铋和铋化合物的化学潜能得到了积极的开发。铋盐的毒性较低,因此它们可能成为大规模合成的有价值的试剂,在处理活性药物成分或合成中间体等产品时,这一点更为明显。相反,铋化合物在医学中得到了广泛的应用。在现代抗生素出现之前,铋化合物曾被广泛用于梅毒和其他细菌感染的治疗,而现在它们仍然是治疗几种胃肠道疾病的重要药物,此外,铋化合物还具有抗菌和细胞毒性活性等特性。本文综述了过去几年中铋试剂和催化剂在用于制备具有药用价值的化合物的创新合成工艺中的应用,以及铋化合物的制备、生物学评价和潜在药用用途方面的相关进展。

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