Burger's Medicinal Chemistry and Drug Discovery, Cardiovascular Agents and Endocrines PDF
Preview Burger's Medicinal Chemistry and Drug Discovery, Cardiovascular Agents and Endocrines
BURGER'S MEDICINAL CHEMISTRY AND DRUG DISCOVERY 4 Sixth Edition Volume 3: Cardiovascular Agents and Endocrines Edited by Donald J. Abraham Department of Medicinal Chemistry School of Pharmacy Virginia Commonwealth University Richmond, Virginia WILEY- INTERSCIENCE A john Wiley and Sons, Inc., Publication PREFACE , Editors, Editorial Board Members, and sixth edition, we devote an entire subsection Wiley and Sons have worked for three of Volume 4 to cancer research; we have also a half years to update the fifth edition of reviewed the major published Medicinal ger's Medicinal Chemistry and Drug Dis- Chemistry and Pharmacology texts to ensure wvery. The sixth edition has several new and that we did not omit any major therapeutic unique features. For the first time, there will classes of drugs. An editorial board was consti- an online version of this major reference tuted for the first time to also review and sug- rk. The online version will permit updating gest topics for inclusion. Their help was and easy access. For the first time, all volumes greatly appreciated. The newest innovation in are structured entirely according to content this series will be the publication of an aca- and published simultaneously. Our intention demic, "textbook-like" version titled, "Bur- was to provide a spectrum of fields that would ger's Fundamentals of Medicinal Chemistry." new or experienced medicinal chem- The academic text is to be published about a biologists, pharmacologists and molecu- year after this reference work appears. It will iologists entry to their subjects of interest also appear with soft cover. Appropriate and as well as provide a current and global per- key information will be extracted from the ma- spective of drug design, and drug develop- jor reference. There are numerous colleagues, friends, Our hope was to make this edition of and associates to thank for their assistance. Burger the most comprehensive and useful First and foremost is Assistant Editor Dr. published to date. To accomplish this goal, we John Andrako, Professor emeritus, Virginia expanded the content from 69 chapters (5 vol- Commonwealth University, School of Phar- es) by approximately 50% (to over 100 macy. John and I met almost every Tuesday s in 6 volumes). We are greatly in debt for over three years to map out and execute thors and editorial board members the game plan for the sixth edition. His contri- icipating in this revision of the major ref- bution to the sixth edition cannot be under- work in our field. Several new subject stated. Ms. Susanne Steitz, Editorial Program ave emerged since the fifth edition ap- Coordinator at Wiley, tirelessly and meticu- Proteomics, genomics, bioinformatics, lously kept us on schedule. Her contribution mbinatorial chemistry, high-throughput was also key in helping encourage authors to screening, blood substitutes, allosteric effec- return manuscripts and revisions so we could tors as potential drugs, COX inhibitors, the publish the entire set at once. I would also like etatins, and high-throughput pharmacology to especially thank colleagues who attended are only a few. In addition to the new areas, we the QSAR Gordon Conference in 1999 for very have filled in gaps in the fifth edition by in- helpful suggestions, especially Roy Vaz, John cluding topics that were not covered. In the Mason, Yvonne Martin, John Block, and Hugo Preface Kubinyi. The editors are greatly indebted to Dukat, Martin Safo, Jason Rife, Kevin k e p - Professor Peter Ruenitz for preparing a tem- olds, and John Andrako in our Department plate chapter as a guide for all authors. My of Medicinal Chemistry, School of Pharmacy, secretary, Michelle Craighead, deserves spe- Virginia Commonwealth University for sug- cial thanks for helping contact authors and gestions and special assistance in reviewing reading the several thousand e-mails gener- manuscripts and text. Graduate student ated during the project. I also thank the com- Derek Cashman took able charge of our web puter center at Virginia Commonwealth Uni- site, http://www.burgersmedchem.com, an- versity for suspending rules on storage and other first for this reference work. I would es- e-mail so that we might safely store all the pecially like to thank my dean, Victor versions of the author's manuscripts where Yanchick, and,Virginia Commonwealth Uni- they could be backed up daily. Last and not versity for their support and encouragement, least, I want to thank each and every author, Finally, I thank my wife Nancy who under- some of whom tackled two chapters. Their stood the magnitude of this project and pro- contributions have provided our field with a vided insight on how to set up our home office sound foundation of information to build for as well as provide John Andrako and me the future. We thank the many reviewers of lunchtime menus where we often dreamed of " manuscripts whose critiques have greatly en- getting chapters completed in all areas we se- hanced the presentation and content for the lected. To everyone involved, many, many sixth edition. Special thanks to Professors thanks. Richard Glennon, William Soine, Richard Westkaemper, Umesh Desai, Glen Kel- DONALD J. ABRAHAM logg, Brad Windle, Lemont Kier, Malgorzata Midlothian, Virginia Dr. Alfred Burger rhotograph or Professor Burger followed by his comments to the American Chemical Society 26th Medicinal Chemistry Symposium on June 14, 1998. This was his last public appearance at a meeting of medicinal chemists. As general chair of the 1998 ACS Medicinal Chemistry Symposium, the editor invited Professor Burger to open the meeting. He was concerned that the young chemists would not know who he was and he might have an attack due to his battle with Parkinson's disease. These fears never were realized and his comments to the more than five hundred attendees drew a sustained standing ovation. The Professor was 93, and it was Mrs. Burger's 91st birthday. Opening Remarks ACS 26th Medicinal Chemistry Symposium June 14, I998 Alfred Burger University of Virginia It has been 46 years since the third Medicinal Chemistry Symposium met at the University of Virginia in Charlottesville in 1952. Today, the Virginia Commonwealth University welcomes you and joins all of you in looking forward to an exciting program. So many aspects of medicinal chemistry have changed in that half century that most of the new data to be presented this week would have been unexpected and unbelievable had they been mentioned in 1952. The upsurge in biochemical understandings of drug transport and drug action has made rational drug design a reality in many therapeutic areas and has made medicinal chemistry an independent science. We have our own journal, the best in the world, whose articles comprise all the innovations of medicinal researches. And if you look at the announcements of job opportunities in the pharmaceutical industry as they appear in Chemical & Engineering News, you will find in every issue more openings in medicinal &emistry than in other fields of chemistry. Thus, we can feel the excitement of being part of this medicinal tidal wave, which has also been fed by the expansion of the needed research training provided by increasing numbers of universities. The ultimate beneficiary of scientific advances in discovering new and better therapeutic agents and understanding their modes of action is the patient. Physicians now can safely look forward to new methods of treatment of hitherto untreatable conditions. To the medicinal scientist all this has increased the pride of belonging to a profession which can offer predictable intellectual rewards. Our symposium will be an integral part of these developments. xii CONTENTS 1 CARDIAC DRUGS: 3 MYOCARDIAL INFARCTION ANTIANGINAL, VASODILATORS, AGENTS, 155 ANTIARRHYTHMIC, 1 George E. Billman Gajanan S. Joshi Ruth A. Altschuld Allos Therapeutics, Inc. The Ohio State University Westminster, Colorado Columbus, Ohio James C. Burnett Virginia Commonwealth University 4 ENDOGENOUS VASOACTIVE Richmond, Virginia PEPTIDES, 193 Donald J. Abraham James L. Stanton Institute for Structural Biology and Randy L. Webb Drug Discovery Metabolic and Cardiovascular School of Pharmacy and Diseases Department of Medicinal Chemistry Novartis Institute for Biomedical Virginia Commonwealth University Research Richmond, Virginia Summit, New Jersey 2 DIURETIC AND URICOSURIC 5 HEMATOPOIETIC AGENTS, 251 AGENTS, 55 Maureen Harrington Cynthia A. Fink Indiana University Jeffrey M. McKenna Walther Oncology Center Lincoln H. Werner Indianapolis, Indiana Novartis Biomedical Research Institute 6 ANTICOAGULANTS, Metabolic and Cardiovascular ANTITHROMBOTICS, AND Diseases Research HEMOSTATICS, 283 Summit, New Jersey Gregory S. Bisacchi Bristol-Myers Squibb Princeton, New Jersey xiii . xiv Contents 7 ANTIHYPERLIPIDEMIC 10 IRON CHELATORS AND AGENTS, 339 THERAPEUTIC USES, 479 Michael L. Sierra Raymond J. Bergeron Centre de Recherches James S. McManis Laboratoire GlaxoSmithKline William R. Weimar Les Ulis, France Jan Wiegand Eileen Eiler-McManis College of Pharmacy 8 OXYGEN DELIVERY BY University of Florida ALLOSTERIC EFFECTORS OF Gainesville, Florida HEMOGLOBIN, BLOOD SUBSTITUTES, AND PLASMA EXPANDERS, 385 11 THYROID HORMONES AND THYROMIMETICS, 563 Barbara Campanini Stefano Bruno Denis E. Ryono Samanta Raboni Discovery Chemistry Andrea Mozzarelli Gary J. Grover Department of Biochemistry and Metabolic Diseases Biology Molecular Biology Bristol-Myers Squibb National Institute for the Physics of Princeton, New Jersey Matter University of Parma Karin Mellstrom Parma, Italy Cell Biology Karo Bio AB Huddinge, Sweden 9 INHIBITION OF SICKLE HEMOGLOBIN POLYMERIZATION AS A BASIS 12 FUNDAMENTALS OF STEROID FOR THERAPEUTIC APPROACH CHEMISTRY AND TO SICKLE-CELL ANEMIA, 443 BIOCHEMISTRY, 593 Constance Tom Noguchi Robert W. Brueggemeier Alan N. Schechter Pui-kai Li National Institute of Diabetes, Division of Medicinal Chemistry Digestive and Kidney Diseases, and Pharmacognosy National Institutes of Health College of Pharmacy Laboratory of Chemical Biology The Ohio State University Bethesda, Maryland Columbus, Ohio John D. Haley 13 FEMALE SEX HORMONES, OSI Pharmaceuticals Inc. CONTRACEPTIWS, AND Uniondale, New York FERTILITY DRUGS, 629 Donald J. Abraham Peter C. Ruenitz Virginia Commonwealth University College of Pharmacy Department of Medicinal Chemistry University of Georgia Richmond, Virginia Athens, Georgia Contents 14 MALE SEX HORMONES, 15 ANTI-INFLAMMATORY ANALOGS, AND ANTAGONISTS, STEROIDS, 747 679 Mitchell A. Avery John R. Woolfrey Robert W. Brueggemeier University of Mississippi-University Division of Medicinal Chemistry Department of Medicinal Chemistry and Pharmacognosy School of Pharmacy The Ohio State University, College University, Mississippi of Pharmacy Columbus, Ohio INDEX, 881 BURGER'S MEDICINAL CHEMISTRY A N D D R U G DISCOVERY
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