Johnson Nicholas A, Southerland Marie R, Youngs Wiley J
Department of Chemistry, 401 College Ave., Ashland University, Ashland, OH 44805, USA.
Department of Chemistry, University of Akron, Akron, OH 44325, USA.
Molecules. 2017 Jul 27;22(8):1263. doi: 10.3390/molecules22081263.
Because of their great structural diversity and multitude of chemical properties, N-heterocyclic carbenes (NHCs) have been utilized in a variety of capacities. Most recently, NHCs have been utilized as carrier molecules for many transition metals in medicinal chemistry. Specifically, Ag(I)-NHCs have been investigated as potent antibacterial agents and chemotherapeutics and have shown great efficacy in both in vitro and in vivo studies. Ag(I)-NHC compounds have been shown to be effective against a wide range of both Gram-positive and Gram-negative bacterial strains. Many compounds have also shown great efficacy as antitumor agents demonstrating comparable or better antitumor activity than standard chemotherapeutics such as cisplatin and 5-fluorouracil. While these compounds have shown great promise, clinical use has remained an unattained goal. Current research has been focused upon synthesis of novel Ag(I)-NHC compounds and further investigations of their antibacterial and antitumor activity. This review will focus on recent advances of Ag(I)-NHCs in medicinal applications.
由于其巨大的结构多样性和众多的化学性质,N-杂环卡宾(NHCs)已被用于多种用途。最近,NHCs在药物化学中被用作许多过渡金属的载体分子。具体而言,Ag(I)-NHCs已被研究作为强效抗菌剂和化疗药物,并在体外和体内研究中均显示出巨大的疗效。Ag(I)-NHC化合物已被证明对多种革兰氏阳性和革兰氏阴性细菌菌株有效。许多化合物作为抗肿瘤剂也显示出巨大的疗效,其抗肿瘤活性与顺铂和5-氟尿嘧啶等标准化疗药物相当或更好。虽然这些化合物已显示出巨大的前景,但临床应用仍然是一个未实现的目标。目前的研究集中在新型Ag(I)-NHC化合物的合成及其抗菌和抗肿瘤活性的进一步研究上。本综述将重点关注Ag(I)-NHCs在医学应用中的最新进展。