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多供体杂环硫代酰胺的银衍生物作为抗菌/抗癌剂:对耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌和人骨肉瘤细胞系具有异常的生物活性。

Silver derivatives of multi-donor heterocyclic thioamides as antimicrobial/anticancer agents: unusual bio-activity against methicillin resistant , , and and human bone cancer cell line.

作者信息

Aulakh Jaspreet K, Lobana Tarlok S, Sood Henna, Arora Daljit S, Kaur Raminderjit, Singh Jatinder, Garcia-Santos Isabel, Kaur Manpreet, Jasinski Jerry P

机构信息

Department of Chemistry, Guru Nanak Dev University Amritsar-143 005 India

Department of Microbiology, Guru Nanak Dev University Amritsar-143 005 India.

出版信息

RSC Adv. 2019 May 17;9(27):15470-15487. doi: 10.1039/c9ra01804b. eCollection 2019 May 14.

DOI:10.1039/c9ra01804b
PMID:35514853
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9066168/
Abstract

The basic aim of this study pertains to the synthesis of silver nitrate complexes and the study of their antimicrobial and anticancer bio-activity. A series of new silver(i) derivatives of -substituted-imidazolidine-2-thiones (L-NR, R = Et, Pr , Bu , Ph), purine-6-thione (purSH), 2-thiouracil (tucH), pyrimidine-2-thione (pymSH) and pyridine-2-thione (pySH) of composition [Ag(S-L-NR)(PPh)(ONO)] {R = Et (1), Pr (2), Bu (3), Ph (4)}, Ag(N,S-purSH)(μ-dppm)·2HO (5) (dppm = PhP-CH-PPh), Ag(L)(PPh) {L = N,S-purSH (6); S-tucH (7)}, Ag(N,S-pymS)(PPh) (8), and [Ag(N,S-pyS)(PPh)] (9) have been synthesized and structurally characterized. These new and some previously reported complexes {Ag(L-NH)(PPh) (10), Ag(L-NMe)(PPh) (11), and Ag(S-bzimSH)(PPh) (12), L-NH = 1,3-imidazolidine-2-thione; L-NMe = 1-methyl-3-imidazolidine-2-thione and bzimSH = benzimidazoline-2-thione)} have shown moderate to high anti-microbial activity against Gram positive bacteria, namely methicillin resistant (MRSA) and (MTCC 740), and Gram negative bacteria, namely (MTCC 435), (MTCC 439), (MTCC 1457) and a yeast (MTCC 22). These complexes have also been found to be bio-safe as studied using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] assay. The anti-tumor study of silver complexes against human osteosarcoma cell line (MG63) has shown IC values in the range of 6-33 μM.

摘要

本研究的基本目的是合成硝酸银配合物并研究其抗菌和抗癌生物活性。已合成并通过结构表征得到了一系列新的银(I)衍生物,包括 - 取代 - 咪唑烷 - 2 - 硫酮(L - NR,R = 乙基、丙基、丁基、苯基)、嘌呤 - 6 - 硫酮(purSH)、2 - 硫代尿嘧啶(tucH)、嘧啶 - 2 - 硫酮(pymSH)和吡啶 - 2 - 硫酮(pySH)的配合物,其组成分别为[Ag(S - L - NR)(PPh)(ONO)] {R = 乙基 (1)、丙基 (2)、丁基 (3)、苯基 (4)},Ag(N,S - purSH)(μ - dppm)·2HO (5)(dppm = PhP - CH - PPh),Ag(L)(PPh) {L = N,S - purSH (6); S - tucH (7)},Ag(N,S - pymS)(PPh) (8),以及[Ag(N,S - pyS)(PPh)] (9)。这些新的以及一些先前报道的配合物{Ag(L - NH)(PPh) (10),Ag(L - NMe)(PPh) (11),以及Ag(S - bzimSH)(PPh) (12),L - NH = 1,3 - 咪唑烷 - 2 - 硫酮;L - NMe = 1 - 甲基 - 3 - 咪唑烷 - 2 - 硫酮且bzimSH = 苯并咪唑啉 - 2 - 硫酮}对革兰氏阳性菌,即耐甲氧西林金黄色葡萄球菌(MRSA)和(MTCC 740),以及革兰氏阴性菌,即(MTCC 435)、(MTCC 439)、(MTCC 1457)和酵母(MTCC 22)显示出中度至高的抗菌活性。使用MTT [3 - (4,5 - 二甲基噻唑 - 2 - 基) - 2,5 - 二苯基溴化四氮唑] 试验研究发现这些配合物也是生物安全的。银配合物对人骨肉瘤细胞系(MG63)的抗肿瘤研究显示其IC值在6 - 33 μM范围内。

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