Singh Amandeep, Fong Grant, Liu Jenny, Wu Yun-Hsuan, Chang Kevin, Park William, Kim Jihwan, Tam Christina, Cheng Luisa W, Land Kirkwood M, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
Department of Biological Sciences, University of the Pacific, Stockton, California 95211, United States.
ACS Omega. 2018 May 31;3(5):5808-5813. doi: 10.1021/acsomega.8b00553. Epub 2018 May 30.
In this study, we outline the synthesis of isatin-ferrocenyl chalcone and 1-1,2,3-triazole-tethered isatin-ferrocene conjugates along with their antimicrobial evaluation against the human mucosal pathogen . The introduction of a triazole ring among the synthesized conjugates improved the activity profiles with most of the compounds in the library, exhibiting 100% growth inhibition in a preliminary susceptibility screen at 100 μM. IC determination of the most potent compounds in the set revealed an inhibitory range between 2 and 13 μM. Normal flora microbiome are unaffected by these compounds, suggesting that these may be new chemical scaffolds for the discovery of new drugs against trichomonad infections.
在本研究中，我们概述了异吲哚酮-二茂铁基查尔酮和1,2,3-三唑连接的异吲哚酮-二茂铁共轭物的合成，以及它们对人类黏膜病原体的抗菌评估。在合成的共轭物中引入三唑环改善了活性谱，库中的大多数化合物在100 μM的初步药敏筛选中表现出100%的生长抑制。对该组中最有效的化合物进行IC测定，结果显示抑制范围在2至13 μM之间。正常菌群微生物群不受这些化合物的影响，这表明它们可能是发现抗滴虫感染新药的新化学支架。
