Medicinal Chemistry and Pharmaceutics Core

项目总结： 药物化学和药物制剂学核心将由帕特里克·辛科博士领导，帕克- 戴维斯药学院药剂学和药物输送教授兼副教授 罗格斯大学研究部主任。Sinko博士以他在机械方面的专业知识而闻名 药物动力学和生物药剂学；药物和药物类似物的运输和代谢 天然化合物、药物靶向、生物利用度以及药物的口服和脑内给药 大分子和生物偶联递送载体。与霍华德·S·邦恩的内德·海因德尔合作 利哈伊大学化学教授，他将直接与研究和研究人员互动 硫磺芥菜开发项目评价对策。内德·海因德尔博士的专业知识在 药物化学和小分子有机化合物的合成。海因德尔博士持有11 候选药物的专利，其中一项转让给ICN公司(一种治疗牛皮癣的药物) 其中三种授权给Baxter公司(抗病毒药物)。他目前担任的承包商是 Azevan PharmPharmticals，一家风险投资初创公司，在那里他指导药物-有机合成 该计划已经产生了一系列有希望的新临床候选对象，这些候选对象选择性地阻止了 精氨酸加压素的作用。他在支持商业药物方面有40年的学术研发历史 发展。辛科博士和海因德尔博士都在药物化学、药物配方和 医药药品开发。药物化学小组将参与药物的合成 包括结构类似物在内的先导化合物需要识别活性药效团并优化 进一步发展的对策。同样重要的是扩大候选Lead的合成 用于动物研究的化合物。制药集团将主要专注于优化交付 针对目标组织的对策，同时将毒性降至最低。他们的战略将是ADME/PK测试 产生的化合物，如果在体外结果令人满意，它们将在体内进行测试。如果化合物失效，他们就会 可以使用Sinko博士实验室提供的先进药物输送系统重新配制。这 假设失败是交付能力差的结果--这通常是事实。如果对策是 成功在体内，然后使IND的研究将与药理学和 药物开发核心。

Project Summary: The Medicinal Chemistry and Pharmaceutics Core will be headed by Dr. Patrick Sinko, the Parke- Davis Professor of Pharmaceufics and Drug Delivery in the School of Pharmacy and Associate Vice President for Research at Rutgers University. Dr. Sinko is well known for his expertise in mechanismbased pharmacokinefics and biopharmaceutics; transport and metabolism of drugs and drug analogues of natural compounds, drug targeting, bioavailability, and the oral and brain delivery of pharmaceufical macromolecules and bioconjugate delivery vehicles. Working with Ned Heindel, the Howard S. Bunn Professor of Chemistry at Lehigh University, he will directly interact with investigators in the Research and Development Projects evaluating countermeasures to sulfur mustard. Dr. Ned Heindel's expertise is in medicinal chemistry and the synthesis of small molecular weight organic compounds. Dr. Heindel holds 11 patents on candidate pharmaceuticals, one of which was transferred to ICN Corporation (an antipsoriatic) and three of which are licensed to Baxter Corporation (antivirals). He currently serves as a contractor for Azevan Pharmaceuticals, a venture capital start-up, where he directs the medicinal-organic synthesis program which has generated a series of promising novel clinical candidates which selectively block the effects of arginine vasopressin. He has a 40 year history of academic R&D in support of commercial drug development. Both Drs. Sinko and Heindel have expertise in medicinal chemistry, drug formulations and pharmaceutical drug development. The Medicinal Chemistry group will be involved in synthesis of drug leads including structural analogs needed to identify active pharmacophores and to optimize countermeasures forfurther development. Also important will be scale-up synthesis of candidate lead compounds for animal studies. The Pharmaceufics group will be primarily focused on opfimizing delivery of countermeasures to target tissues while minimizing toxicity. Their strategy will be ADME/PK tesfing of compounds generated, if results are satisfactory in vitro, they will be tested in vivo. If compounds fail, they can be reformulated using advanced drug delivery systems available in Dr. Sinko's laboratory. This assumes that failure is a result of poor deliverability- which is often the case. If countermeasures are successful in vivo, then IND-enabling studies will be performed in collaboration with the Pharmacology and Drug Development Core.