吡嗪酰胺与{金（I）-三苯基膦}部分共轭后对结核分枝杆菌的杀菌作用增强。 （注：原文toward后缺少具体对象，根据常见医学语境推测补充了“结核分枝杆菌”，以使译文完整通顺，若有特殊要求请按要求调整）
Enhanced Bactericidal Effects of Pyrazinamide Toward and upon Conjugation to a {Au(I)-triphenylphosphine} Moiety.
作者信息
Stenger-Smith Jenny, Kamariza Mireille, Chakraborty Indranil, Ouattara Ramatoulaye, Bertozzi Carolyn R, Mascharak Pradip K
机构信息
Department of Chemistry and Biochemistry, University of California, Santa Cruz, California 95064, United States.
Department of Chemistry, Stanford University, Stanford, California 94305, United States.
出版信息
ACS Omega. 2020 Mar 18;5(12):6826-6833. doi: 10.1021/acsomega.0c00071. eCollection 2020 Mar 31.
As part of the quest for new gold drugs, we have explored the efficacy of three gold complexes derived from the tuberculosis drug pyrazinamide (PZA), namely, the gold(I) complex [Au(PPh)(PZA)]OTf (, OTf = trifluoromethanesulfonate) and two gold(III) complexes [Au(PZA)Cl] () and [Au(PZO)Cl] (, PZO = pyrazinoic acid, the metabolic product of PZA) against two mycobacteria, and . Only complex with the {Au(PPh)} moiety exhibits significant bactericidal activity against both strains. In the presence of thiols, gives rise to free PZA and {Au(PPh)}-thiol polymeric species. A combination of PZA and the {Au(PPh)}-thiol polymeric species appears to lead to enhanced efficacy of against .
作为探索新型金药物的一部分，我们研究了三种源自抗结核药物吡嗪酰胺（PZA）的金配合物的疗效，即金（I）配合物[Au(PPh)(PZA)]OTf（OTf = 三氟甲磺酸盐）以及两种金（III）配合物[Au(PZA)Cl]（ ）和[Au(PZO)Cl]（PZO = 吡嗪酸，PZA的代谢产物）对两种分枝杆菌 和 的作用。只有具有{Au(PPh)}部分的配合物 对两种菌株均表现出显著的杀菌活性。在硫醇存在的情况下， 会产生游离的PZA和{Au(PPh)}-硫醇聚合物物种。PZA与{Au(PPh)}-硫醇聚合物物种的组合似乎会导致 对 的疗效增强。
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