Koza, Darrell J. - Eastern Connecticut State University

个人简介

B.S. Chemistry, University of Rhode Island Ph.D. Organic Chemistry, University of Rhode Island Postdoctoral, Tufts University Medical School

研究领域

Since the discovery of penicillin in 1928 microbes have appeared that can resist the effects of this powerful class of antibiotics. By the end of the 1940’s a large majority of bacteria had acquired resistance to penicillin as well as chemical cousins methicillin and oxacillin. Antibiotic resistant bacteria have a substantial impact on the treatment of infections. Even today, many bacteria are resistant to one or more of the 100 antibiotics in use and some strains are resistant to the “antibiotics of last resort” ; vancomycin and fluoroquinolones. The “coming plague” of multi-antibiotic resistant bacteria is fought by chemists and biologists in the laboratory everyday. Research efforts in our laboratory focus on the synthesis of small molecule inhibitors of bacterial resistance mechanisms. Towards this goal we utilize contemporary transition metal catalyzed reactions for synthesizing derivatives of lead compounds. Our chemistry efforts are strongly integrated and guided by the biological evaluation of our synthetic derivatives in hopes that this will lead to a new class of antibiotics effective for the treatment of infections caused by multi-anibiotic resistant (MAR) microorganisms.

近期论文

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A Convenient Synthesis of 2,2′ Biindole. Darrell J. Koza and William B. EulerHeterocyclic Communications, 1999, 5, 399 Synthesis of 7-Substituted Tetracycline Derivatives. Darrell J. Koza.Organic Letters, 2000, 6, 815. Synthesis of 8-Substituted Tetracyclines, The First 8-Position Carbon-Carbon Bond. Darrell J. Koza.Tetrahedron Letters, 2000, 26, 5017. Synthesis and Biological Evaluation of 9-Substituted Tetracycline Derivatives. Darrell J. Koza and Yaw A. Nsiah.Bioorganic and Medicinal Chemistry Letters, 2002, 12, 2163. Palladium Catalyzed C-N Bond Formation in the Synthesis of 7-Amino Substituted Tetracyclines. Darrell J. Koza and Yaw A. Nsiah.Journal of Organic Chemistry, 2002, 67, 5025. An Efficient High Yielding Approach for the Homocoupling of Aryl Boronic Acids. Darrell J. Koza and Eric Carita.Synthesis, 2002, 15, 2183. Koza, Darrell J. and Nelson, Mark L. “7, 8, and 9-Substituted Tetracycline Compounds.” US Patent 6,624,168. 23 Sept. 2003. Koza, Darrell J., Nelson, Mark L., and Rennie, Glen. “Methods of Preparing Substituted Tetracyclines with Transition Metal Based Chemistries.” US Patent 6,617,318. 9 Sept. 2003. Toedt, J., Koza, D., Van Cleef – Toedt, K. Chemical Composition of Everyday Products.Greenwood Press. Westport. 2005. Koza, Darrell J., Nelson, Mark L., and Rennie, Glen. “Methods of Preparing Substituted Tetracyclines with Transition Metal Based Chemistries.”US Patent 7,067,681. 27 Jun. 2006. Koza, Darrell J., Nelson, Mark L., and Rennie, Glen. “7, 8, and 9-Substituted Tetracycline Compounds.”US Patent 7,094,806. 22 Aug. 2006.