Daniel Lednicer, PhD, is the author of several books on drug synthesis and discovery. His career in both the private and public sectors has been devoted to the search for new therapeutic agents. Dr. Lednicer spent two decades at the bench as a chemist at the Upjohn Company. Following that, he served as director of chemical research at Mead Johnson, director of pharmaceutical sciences at Adria Laboratories, and pharmaceutical manager at Analytical Biochemistry Laboratories. Most recently, he was a project officer at the National Cancer Institute. Lester A. Mitscher, Ph.D., recognized for his research achievements by numerous institutions, serves as a consultant for the National Institutes of Health, among other organizations. Dr. Mitscher is a professor at the University of Kansas and the Victorian College of Pharmacy at Monash University outside Melbourne, Australia. Victoria Dolby Toews, MPH, a veteran freelance researcher and writer, has written and coauthored many books on health and wellness. She lives in the Pacific Northwest.

• Preface xi Open-Chain Compounds 1Peptidomimetic Compounds 2Antiviral Protease Inhibitors 2Human Immunodeficiency Virus 2Human Rhinovirus 9Miscellaneous Peptidomimetic Compounds 11References 19Alicyclic Compounds 21Monocyclic Compounds 21Prostaglandins 21Antiviral Agents 25Miscellaneous Monocyclic Compounds 29Polycyclic Compounds: Steroids 3119-Nor Steroids 31Corticosteroid Related Compounds 34Polycyclic Compounds / 38References 40Monocyclic Aromatic Compounds 43Arylcarbonyl Derivatives 43Biphenyls 47Compounds Related to Aniline 50Compounds Related to Arylsulfonic Acids 53Diarylmethanes 58Miscellaneous Monocyclic Aromatic Compounds 60References 67Carbocyclic Compounds Fused to a Benzene Ring 69Indenes 69Naphthalenes 73Tetrahydronaphthalenes 74Other benzofused carbocyclic compounds 79References 81Five-Membered Heterocycles 83Compounds with One Heteroatom 83Compounds with Two Heteroatoms 91Oxazole and Isoxazoles 91Imidazoles and a Pyrrazole 94Thiazoles 99Triazoles 103Tetrazoles 109References 112Six-Membered Heterocycles 115Compounds with One Heteroatom 115Pyridines 115Reduced Pyridines 117Miscellaneous 119Compounds with Two Heteroatoms 121Pyrimidines 121Miscellaneous Six-Membered Heterocycles 133References 136Five-Membered Heterocycles Fused to One Benzene Ring 139Compounds with One Heteroatom 139Benzofurans 139Indoles 141Indolones 148Miscellaneous Compounds with One Heteroatom 153Five-Membered Rings with Two Heterocyclic Atoms 156Benzimidazoles 156Miscellaneous Compounds  158References 160Six-Membered Heterocycles Fused to One Benzene Ring 163Compounds with One Heteroatom 163Benzopyrans 163Quinolines and Their Derivatives 167Quinolone Antibacterial Agents 172Compounds with Two Heteroatoms 176Benzoxazines 176Quinazolines 178Miscellaneous Benzo-Fused Heterocycles 184References 186Bicyclic Fused Heterocycles 189Compounds with Five-Membered Rings Fused to Six-Membered Rings 189Compounds with Two Heteroatoms 189Compounds with Three Heteroatoms 191Compounds with Four Heteroatoms 195Compounds with Two Fused Six-Membered Rings 208Miscellaneous Compounds with Two Fused Heterocyclic Rings: Beta Lactams 213References 215Polycyclic Fused Heterocycles 217Compounds with Three Fused Rings 217Compounds with Four Fused Rings 228Compounds with Five or More Fused Rings: Camptothecins 230References 232Subject Index 233Cross Index of Biological Activity  241Cumulative Index 245