ORGANOTIN BIOCIDES--SYNTHESIS AND EVALUATION

有机锡杀菌剂——合成与评价

• 批准号: 6107010
• 负责人: KEITH H PANNELL
• 金额: $ 4.04万
• 依托单位: UNIVERSITY OF TEXAS EL PASO
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-06-01 至 2000-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6107010
• 关键词: X ray crystallography; antibacterial agents; antifungal agents; antineoplastics; chemical structure function; chemical substitution; chemical synthesis; computer simulation; drug screening /evaluation; environmental contamination; ferrocene; metal complex; microbiology; nuclear magnetic resonance spectroscopy; organic chemicals; photochemistry; physical model; polymers; silicon; tin

This proposal entails the provision of new, more effective and safe, organotin biocides. The synthesis, chemical and structural characterization, biocidal evaluation and some environmental fate analysis, of a new series of organotins, R3SnX and R2SnX2, that contain mixed functional groups will be performed. All presently known materials are homoleptic, i.e. all R groups are identical. Compounds with new R groups with specific properties (e.g. ionophore character, an important mechanistic property of organotins); systems with mixed R groups (active with less active substituents, e.g. ethyl and octyl groups); and oligonucleotide ligands will be targeted. Synthesis will involve procedures previous developed by the PI. Characterization will include multi-nuclear NMR, single crystal X-ray diffraction, and EXAFS; initial biocidal screening evaluation will involve direct testing against luminous bacteria. Synergistic activities of mixtures of organotins will be evaluated by the bacterial assay. Ionophoric properties with respect to both anion and cation transport will be determined. Promising materials will be further tested on more sophisticated systems via pre- arranged collaborative agreements. All appropriate, safety, handling, training programs and safeguards are in place. Organotins have widespread use against bacteria and fungi, in both agricultural crop production and human health arenas, including specific disease treatments and potential anti-cancer drugs. The properties of the various preparations are very dependent upon the R group present , thus the proposed research will have direct bearing upon the availability of new tools to fight disease and disease carrying pests. Recently it has been recognized that the use of organotins has been hampered by a clear lack of recent research in this field.

这项建议要求提供新的、更有效和安全的有机杀菌剂。本文研究了一类新的含混合官能团的有机化合物R3SnX和R2SnX2的合成、化学性质、结构表征、杀菌剂评价和环境命运分析。所有已知的材料都是同感的，即所有的R群都是相同的。具有特定性质的新R基团的化合物（如离子载体性质，有机锡的重要机理性质）；含有混合R基团（与活性较低的取代基，如乙基和辛基）的体系；寡核苷酸配体将成为目标。综合将涉及PI先前开发的程序。表征将包括多核磁共振、单晶x射线衍射和EXAFS；最初的杀菌剂筛选评估将包括对发光细菌的直接测试。有机物混合物的协同作用将通过细菌试验来评估。关于阴离子和正离子传输的电离电性质将被确定。有前途的材料将通过预先安排的合作协议在更复杂的系统上进一步测试。所有适当的、安全的、处理的、培训的计划和保障措施都到位了。有机锡在农业作物生产和人类健康领域广泛用于对抗细菌和真菌，包括特定疾病治疗和潜在的抗癌药物。各种制剂的性质很大程度上取决于R基团的存在，因此拟议的研究将直接影响到对抗疾病和携带疾病的害虫的新工具的可用性。最近，人们认识到，由于在这一领域明显缺乏最近的研究，有机素的使用受到了阻碍。