Medicinal Chemistry and Pharmaceutics Core

项目摘要： 药物化学和药剂学核心将由帕克-帕特里克辛科博士领导。 戴维斯药学院药剂学和药物输送教授和副教授 罗格斯大学研究部主任。Sinko博士以其在基于机械的 药物动力学和生物药剂学;药物和药物类似物的转运和代谢 天然化合物、药物靶向、生物利用度以及药物的口服和脑内递送 大分子和生物缀合物递送载体。与内德·海因德尔合作，霍华德S。邦恩 利哈伊大学化学教授，他将直接与研究人员互动， 发展项目评估对策硫芥子气。内德·亨德尔博士的专长是 药物化学和小分子量有机化合物的合成。Heindel博士持有11 候选药物的专利，其中一项已转让给ICN公司（一种抗银屑病药） 其中三种被许可给巴克斯特公司（抗病毒药物）。他目前担任承包商， Azevan Pharmaceuticals，一家风险投资初创公司，他在那里指导药物有机合成 该计划已经产生了一系列有前途的新的临床候选人，这些候选人选择性地阻断了 精氨酸加压素的作用。他有40年的学术研发历史，以支持商业药物 发展Sinko博士和Heindel博士都具有药物化学，药物配方和 药物开发。药物化学组将参与药物的合成 先导化合物，包括鉴定活性药效团和优化 进一步发展的对策。同样重要的是扩大候选先导化合物的合成 用于动物研究的化合物。制药组将主要关注优化输送 针对目标组织的对策，同时最大限度地减少毒性。他们的策略将是ADME/PK测试， 如果体外结果令人满意，则将对生成的化合物进行体内测试。如果化合物失效， 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 假设失败是由于交付能力差--这是经常发生的情况。如果反制措施 如果在体内成功，则将与药理学和 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.