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.

"The book is up-to-date with regard to the drugs presented and has the potential to be a good resources for experienced researchers in drug design…" (Journal of the American Chemical Society, March 12, 2008)

• Preface xi1 Open-Chain Compounds 11. Peptidomimetic Compounds 2A. Antiviral Protease Inhibitors 21. Human Immunodeficiency Virus 22. Human Rhinovirus 92. Miscellaneous Peptidomimetic Compounds 11References 192 Alicyclic Compounds 211. Monocyclic Compounds 21A. Prostaglandins 21B. Antiviral Agents 25C. Miscellaneous Monocyclic Compounds 292. Polycyclic Compounds: Steroids 31A. 19-Nor Steroids 31B. Corticosteroid Related Compounds 343. Polycyclic Compounds 38References 403 Monocyclic Aromatic Compounds 431. Arylcarbonyl Derivatives 432. Biphenyls 473. Compounds Related to Aniline 504. Compounds Related to Arylsulfonic Acids 535. Diarylmethanes 586. Miscellaneous Monocyclic Aromatic Compounds 60References 674 Carbocyclic Compounds Fused to a Benzene Ring 691. Indenes 692. Naphthalenes 733. Tetrahydronaphthalenes 744. Other benzofused carbocyclic compounds 79References 815 Five-Membered Heterocycles 831. Compounds with One Heteroatom 832. Compounds with Two Heteroatoms 91A. Oxazole and Isoxazoles 91B. Imidazoles and a Pyrrazole 94C. Thiazoles 99D. Triazoles 103E. Tetrazoles 109References 1126 Six-Membered Heterocycles 1151. Compounds with One Heteroatom 115A. Pyridines 115B. Reduced Pyridines 117C. Miscellaneous 1192. Compounds with Two Heteroatoms 121A. Pyrimidines 121B. Miscellaneous Six-Membered Heterocycles 133References 1367 Five-Membered Heterocycles Fused to One Benzene Ring 1391. Compounds with One Heteroatom 139A. Benzofurans 139B. Indoles 141C. Indolones 148D. Miscellaneous Compounds with One Heteroatom 1532. Five-Membered Rings with Two Heterocyclic Atoms 156A. Benzimidazoles 156B. Miscellaneous Compounds 158References 1608 Six-Membered Heterocycles Fused to One Benzene Ring 1631. Compounds with One Heteroatom 163A. Benzopyrans 163B. Quinolines and Their Derivatives 167C. Quinolone Antibacterial Agents 1722. Compounds with Two Heteroatoms 176A. Benzoxazines 176B. Quinazolines 178C. Miscellaneous Benzo-Fused Heterocycles 184References 1869 Bicyclic Fused Heterocycles 1891. Compounds with Five-Membered Rings Fused to Six-Membered Rings 189A. Compounds with Two Heteroatoms 189B. Compounds with Three Heteroatoms 191C. Compounds with Four Heteroatoms 1952. Compounds with Two Fused Six-Membered Rings 2083. Miscellaneous Compounds with Two Fused Heterocyclic Rings: Beta Lactams 213References 21510 Polycyclic Fused Heterocycles 2171. Compounds with Three Fused Rings 2172. Compounds with Four Fused Rings 2283. Compounds with Five or More Fused Rings: Camptothecins 230References 232Subject Index 233Cross Index of Biological Activity 241Cumulative Index 245

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.

"The book is up-to-date with regard to the drugs presented and has the potential to be a good resources for experienced researchers in drug design…" (Journal of the American Chemical Society, March 12, 2008)

• Preface xi1 Open-Chain Compounds 11. Peptidomimetic Compounds 2A. Antiviral Protease Inhibitors 21. Human Immunodeficiency Virus 22. Human Rhinovirus 92. Miscellaneous Peptidomimetic Compounds 11References 192 Alicyclic Compounds 211. Monocyclic Compounds 21A. Prostaglandins 21B. Antiviral Agents 25C. Miscellaneous Monocyclic Compounds 292. Polycyclic Compounds: Steroids 31A. 19-Nor Steroids 31B. Corticosteroid Related Compounds 343. Polycyclic Compounds 38References 403 Monocyclic Aromatic Compounds 431. Arylcarbonyl Derivatives 432. Biphenyls 473. Compounds Related to Aniline 504. Compounds Related to Arylsulfonic Acids 535. Diarylmethanes 586. Miscellaneous Monocyclic Aromatic Compounds 60References 674 Carbocyclic Compounds Fused to a Benzene Ring 691. Indenes 692. Naphthalenes 733. Tetrahydronaphthalenes 744. Other benzofused carbocyclic compounds 79References 815 Five-Membered Heterocycles 831. Compounds with One Heteroatom 832. Compounds with Two Heteroatoms 91A. Oxazole and Isoxazoles 91B. Imidazoles and a Pyrrazole 94C. Thiazoles 99D. Triazoles 103E. Tetrazoles 109References 1126 Six-Membered Heterocycles 1151. Compounds with One Heteroatom 115A. Pyridines 115B. Reduced Pyridines 117C. Miscellaneous 1192. Compounds with Two Heteroatoms 121A. Pyrimidines 121B. Miscellaneous Six-Membered Heterocycles 133References 1367 Five-Membered Heterocycles Fused to One Benzene Ring 1391. Compounds with One Heteroatom 139A. Benzofurans 139B. Indoles 141C. Indolones 148D. Miscellaneous Compounds with One Heteroatom 1532. Five-Membered Rings with Two Heterocyclic Atoms 156A. Benzimidazoles 156B. Miscellaneous Compounds 158References 1608 Six-Membered Heterocycles Fused to One Benzene Ring 1631. Compounds with One Heteroatom 163A. Benzopyrans 163B. Quinolines and Their Derivatives 167C. Quinolone Antibacterial Agents 1722. Compounds with Two Heteroatoms 176A. Benzoxazines 176B. Quinazolines 178C. Miscellaneous Benzo-Fused Heterocycles 184References 1869 Bicyclic Fused Heterocycles 1891. Compounds with Five-Membered Rings Fused to Six-Membered Rings 189A. Compounds with Two Heteroatoms 189B. Compounds with Three Heteroatoms 191C. Compounds with Four Heteroatoms 1952. Compounds with Two Fused Six-Membered Rings 2083. Miscellaneous Compounds with Two Fused Heterocyclic Rings: Beta Lactams 213References 21510 Polycyclic Fused Heterocycles 2171. Compounds with Three Fused Rings 2172. Compounds with Four Fused Rings 2283. Compounds with Five or More Fused Rings: Camptothecins 230References 232Subject Index 233Cross Index of Biological Activity 241Cumulative Index 245