Combinatorial Synthesis and Screening of Important Classes of Organic Compounds

这一奖项是埃尔曼博士化学博士后奖学金的首次授予。这项工作将开发可能具有生理活性的有机化合物的组合合成方法。组合综合的方法很重要，因为它可以产生比目前的“一次一个”方法多得多的化合物。当需要系统相关的衍生品时，这变得特别有用。要做的工作是在微滴定板上通过氨基二苯甲酮的酰化或烷基化反应生成苯二氮卓类药物。将开发方法来生产更复杂的产品库。目前，合成方法受到一次只能产生一种化合物的事实的限制。这项工作将导致许多相关化合物的同时生产。要研究的方法的发展可以导致更有效和更便宜的方法来治疗人类疾病的重要药物。

This award is the starter grant increment of Dr. Ellman's Postdoctoral Fellowship in Chemistry. The work will develop methods of combinatorial synthesis of organic compounds which may have physiological activity. The approach of combinatorial sythesis is important because it can lead to very many more compounds than the current "one at a time" methods. This becomes particularly useful when systematically related derivatives are desired. The work to be done will lead to benzodiazepines from the acylation or alkylation of amino benzophenones in microtiter plates. Methods will be developed to produce libraries of more complex products. %%% Currently, synthetic methods are limited by the fact that they produce one compound at a time. This work will lead to the simultaneous production of many related compounds. Development of the methods to be studied can lead to much more efficient and less expensive approaches to important drugs for human diseases.