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Silver derivatives of multi-donor heterocyclic thioamides as antimicrobial/anticancer agents: unusual bio-activity against methicillin resistant S. aureus,S. epidermidis,and E. faecalis and human bone cancer MG63 cell line
Authors:Jaspreet K. Aulakh  Tarlok S. Lobana  Henna Sood  Daljit S. Arora  Raminderjit Kaur  Jatinder Singh  Isabel Garcia-Santos  Manpreet Kaur  Jerry P. Jasinski
Affiliation:Department of Chemistry, Guru Nanak Dev University, Amritsar-143 005 India, Fax: +91-183-2258820 ; Department of Microbiology, Guru Nanak Dev University, Amritsar-143 005 India ; Department of Molecular Biology and Biochemistry, Guru Nanak Dev University, Amritsar-143 005 India ; Departamento de Quimica Inorganica, Facultad de Farmacia, Universidad de Santiago, 15782-Santiago Spain ; Department of Chemistry, Keene State College, Keene NH 03435-2001 USA
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 N-substituted-imidazolidine-2-thiones (L-NR, R = Et, Prn, Bun, Ph), purine-6-thione (purSH2), 2-thiouracil (tucH2), pyrimidine-2-thione (pymSH) and pyridine-2-thione (pySH) of composition [Ag(S-L-NR)(PPh3)2(ONO2)] {R = Et (1), Prn (2), Bun (3), Ph (4)}, [Ag2(N,S-purSH2)2(μ-dppm)2](NO3)2·2H2O (5) (dppm = Ph2P–CH2–PPh2), [Ag(L)(PPh3)2](NO3) {L = N,S-purSH2 (6); S-tucH2 (7)}, [Ag(N,S-pymS)(PPh3)2](CH3OH) (8), and [Ag(N,S-pyS)(PPh3)2] (9) have been synthesized and structurally characterized. These new and some previously reported complexes {[Ag2(L-NH)4(PPh3)2](NO3)2 (10), [Ag(L-NMe)2(PPh3)](NO3) (11), and [Ag(S-bzimSH)2(PPh3)2](OAc) (12), L-NH = 1,3-imidazolidine-2-thione; L-NMe = 1-methyl-3-imidazolidine-2-thione and bzimSH2 = benzimidazoline-2-thione)} have shown moderate to high anti-microbial activity against Gram positive bacteria, namely methicillin resistant Staphylococcus aureus (MRSA) and Staphylococcus aureus (MTCC 740), and Gram negative bacteria, namely Staphylococcus epidermidis (MTCC 435), Enterococcus faecalis (MTCC 439), Shigella flexneri (MTCC 1457) and a yeast Candida albicans (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 IC50 values in the range of 6–33 μM.

A series of biosafe mixed-ligand complexes of silver with heterocyclic thioamides have been studied for their antimicrobial/anticancer activity.
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