ORGANOTIN BIOCIDES--SYNTHESIS AND EVALUATION

这项提议需要提供新的、更有效和更安全的有机锡杀菌剂。将进行一系列新的含有混合官能团的有机锡R3SnX和R2SnX2的合成、化学和结构表征、生物活性评价和一些环境归宿分析。所有目前已知的材料都是同质的，即所有的R基团都是相同的。具有特殊性质的新R基团的化合物(例如，离子载体特性，有机锡的重要机械特性)；具有混合R基团的体系(活性与较不活跃的取代基，例如乙基和辛基)；以及寡核苷酸配体将成为目标。综合将涉及由PI以前开发的程序。鉴定将包括多核核磁共振、单晶X射线衍射和EXAFS；初步的生物杀灭筛选评估将包括针对发光细菌的直接测试。有机锡混合物的协同活性将通过细菌试验进行评估。关于阴离子和阳离子传输的离子传递性质将被确定。有希望的材料将通过预先安排的合作协议在更复杂的系统上进行进一步测试。所有适当的、安全的、搬运的、培训计划和保障措施都已到位。有机锡在农作物生产和人类健康领域具有广泛的抗细菌和真菌用途，包括特定的疾病治疗和潜在的抗癌药物。各种制剂的性质非常依赖于存在的R基团，因此，拟议的研究将直接关系到抗击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，有机锡的使用受到了这一领域最新研究的明显缺乏的阻碍。

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.