DuChane Christine M, Karpin George W, Ehrich Marion, Falkinham Joseph O, Merola Joseph S
Virginia Tech Center for Drug Discovery , Blacksburg , VA 24061 , USA . Email:
Department of Chemistry , Virginia Tech , Blacksburg , VA 24061 , USA.
Medchemcomm. 2019 May 14;10(8):1391-1398. doi: 10.1039/c9md00140a. eCollection 2019 Aug 1.
A new class of piano-stool iridium complexes with 1,2-diaminoethane ligands are shown to be effective and safe antimicrobials with activity against , including various isolates of methicillin-resistant strains (MRSA). Comparison to other piano stool complexes with activity against mycobacteria are made along with a discussion of structure-activity relationships. The structures of one the most active complexes with the ligand -1,2-diaminocyclohexane and one of the least active complexes with the ligand -1,2-diaminocyclohexane are compared and discussed with respect to their drastically different activities. toxicity studies for all of the complexes are described. In addition, a mouse study with one of the complexes, [(pentamethylcyclopentadienyl)(-1,2-diaminocyclohexane)(chloro)iridium]chloride, showed no ill effects on the mice at high doses.
一类新型的带有1,2 - 二氨基乙烷配体的钢琴凳型铱配合物被证明是有效且安全的抗菌剂,对包括各种耐甲氧西林菌株(MRSA)分离株在内的多种细菌具有活性。文中将其与其他对分枝杆菌有活性的钢琴凳型配合物进行了比较,并讨论了构效关系。比较并讨论了配体为 - 1,2 - 二氨基环己烷的活性最高的一种配合物和活性最低的一种配合物的结构及其截然不同的活性。描述了所有配合物的毒性研究。此外,对其中一种配合物,即氯化[(五甲基环戊二烯基)( - 1,2 - 二氨基环己烷)(氯)铱]进行的小鼠研究表明,高剂量时对小鼠没有不良影响。