The chemistry of heterocycles is an important branch of organic chemistry. This is due to the fact that a large number of natural products, e. g. hormones, antibiotics, vitamins, etc. are composed of heterocyclic structures. Often, these compounds show beneficial properties and are therefore applied as pharmaceuticals to treat diseases or as insecticides, herbicides or fungicides in crop protection. This volume presents important pharmaceuticals. Each of the 20 chapters covers in a concise manner one class of heterocycles, clearly structuredas follows: * Structural formulas of most important examples (market products) * Short background of history or discovery * Typical syntheses of important examples * Mode of action * Characteristic biological activity * Structure-activity relationship * Additional chemistry information (e.g. further transformations, alternative syntheses, metabolic pathways, etc.) * References. A valuable one-stop reference source for researchers in academia and industry as well as for graduate students with career aspirations in the pharmaceutical chemistry.

Jurgen Dinges obtained his M.S. degree in organic chemistry at the Technical University in Darmstadt, Germany in 1988. He then joined the group of Prof. Frieder W. Lichtenthaler at the same University, where he received his Ph.D. degree in organic chemistry and chemical engineering in 1991. After being awarded a Feodor-Lynen scholarship from the Humboldt foundation, he spent 18 months as a postdoctoral fellow in the group of Prof. William G. Dauben at the University of California at Berkeley, U.S.A. In 1993, Jurgen Dinges joined the department for biochemistry at Syntex, U.S.A. and since 1995 he is working in the pharmaceutical research department at Abbott Laboratories, U.S.A. In 2009, he was a guest editor for Current Topics in Medicinal Chemistry for a special issue on Parkinson's disease. He is an author of 17 publications and 23 patents and a co-inventor of more than 10 clinical drug development candidates. Clemens Lamberth is a senior team leader in the crop protection research department of Syngenta AG, Switzerland. He studied chemistry at the Technical University of Darmstadt, Germany, where he obtained his Ph.D. under the supervision of Prof. Bernd Giese in 1990. Subsequently, he spent one and a half years as a postdoctoral fellow in the group of Prof. Mark Bednarski at the University of California at Berkeley, U.S.A. In 1992 Clemens Lamberth joined the agrochemical research department of Sandoz Agro AG, Switzerland, which is today, after two mergers, part of Syngenta Crop Protection AG. Since 20 years he is specialized in fungicide discovery. He was the organizer of the two-day session 'New Trends for Agrochemicals' at the 2nd EUCHEMS congress in Torino 2008. He is the author of 46 publications and 56 patents and the inventor of Syngenta's fungicide mandipropamid (Revus?, Pergado?).

IINTRODUCTION THE SIGNIFICANCE OF HETEROCYCLES FOR PHARMACEUTICALS AND AGROCHEMICALS Introduction Heterocycles as Framework of Biologically Active Compounds Fine-Tuning the Physicochemical Properties with Heterocycles Heterocycles as Prodrugs Heterocycles as Peptidomimetics Heterocycles as Isosteric Replacement of Functional Groups Heterocycles as Isosteric Replacement of Alicyclic Rings Heterocycles as Isosteric Replacement of other Heterocyclic Rings PART I: Neurological Disorders TROPANE-BASED ALKALOIDS AS MUSCARINIC ANTAGONISTS FOR THE TREATMENT OF ASTHMA, OBSTRUCTIVE PULMONARY DISEASE, AND MOTION SICKNESS Introduction History Synthesis Mode of Action Structure?Activity Relationships MORPHINONE-BASED OPIOID RECEPTOR AGONIST ANALGESICS Introduction History Synthesis Mode of Action Structure?Activity Relationship BARBITURIC ACID-BASED GABA(A) RECEPTOR MODULATORS FOR THE TREATMENT OF SLEEP DISORDER AND EPILEPSY AND AS ANESTHETICS Introduction History Synthesis Mode of Action Structure?Activity Relationship PHENOTHIAZINE-BASED DOPAMINE D2 ANTAGONISTS FOR THE TREATMENT OF SCHIZOPHRENIA Introduction History Synthesis Mode of Action Structure?Activity Relationships ARYLPIPERAZINE-BASED 5-HT1A RECEPTOR PARTIAL AGONISTS AND 5-HT2A ANTAGONISTS FOR THE TREATMENT OF AUTISM, DEPRESSION, ANXIETY, PSYCHOSIS, AND SCHIZOPHRENIA Introduction History Synthesis Mode of Action Structure?Activity Relationship ARYLPIPERIDINE-BASED DOPAMINE D2 ANTAGONISTS/5-HT2A ANTAGONISTS FOR THE TREATMENT OF AUTISM, DEPRESSION, SCHIZOPHRENIA, AND BIPOLAR DISORDER Introduction History Synthesis Mode of Action Structure?Activity Relationship DIBENZAZEPINE-BASED SODIUM CHANNEL BLOCKERS FOR THE TREATMENT OF NEUROPATHIC PAIN Introduction History Synthesis Mode of Action Structure?Activity Relationships PART II: Cardiovascular Diseases DIHYDROPYRIDINE-BASED CALCIUM CHANNEL BLOCKERS FOR THE TREATMENT OF ANGINA PECTORIS AND HYPERTENSION Introduction History Synthesis Mode of Action Structure?Activity Relationship TETRAZOLE-BASED ANGIOTENSIN II TYPE 1 (AT1) ANTAGONISTS FOR THE TREATMENT OF HEART FAILURE AND CONGESTIVE HYPERTENSION Introduction History Synthesis Mode of Action Structure?Activity Relationship THIAZIDE-BASED DIURETICS FOR THE TREATMENT OF HYPERTENSION AND GENITOURINARY DISORDERS Introduction History Synthesis Mode of Action Structure?Activity Relationship TETRAHYDROPYRANONE-BASED HMG-COA REDUCTASE INHIBITORS FOR THE TREATMENT OF ARTERIAL HYPERCHOLESTEROLEMIA Introduction History Synthesis Mode of Action Structure?Activity Relationship PART III: Infectious Diseases ADENINE-BASED REVERSE TRANSCRIPTASE INHIBITORS AS ANTI-HIV AGENTS Introduction History Synthesis Mode of Action Structure?Activity Relationship GUANINE-BASED NUCLEOSIDE ANALOGS AS ANTIVIRAL AGENTS Introduction History Synthesis Mode of Action Structure?Activity Relationship PENICILLIN AND CEPHALOSPORIN ANTIBIOTICS Introduction History Synthesis Mode of Action Structure?Activity Relationships PART IV: Oncology PYRIMIDINE-BASED KINASE INHIBITORS IN CANCER CHEMOTHERAPY Introduction History Synthesis Mode of Action Structure?Activity Relationship BENZYL TRIAZOLE-BASED AROMATASE INHIBITORS FOR THE TREATMENT OF BREAST CANCER Introduction History Synthesis Mode of Action Structure?Activity Relationship PART V: Inflammation and Gastrointestinal Diseases ACETONIDE-BASED GLUCOCORTICOIDS FOR THE TREATMENT OF ASTHMA, SKIN INFLAMMATION AND DISEASES OF THE EYE Introduction History Synthesis Mode of Action Structure?Activity Relationship BENZIMIDAZOLE-BASED H+/K+-ATPASE INHIBITORS FOR THE TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE Introduction History Synthesis Mode of Action Structure?Activity Relationships PART VI: Metabolic Diseases THIAZOLIDINEDIONE-BASED INSULIN SENSITIZERS:PPAR-G AGONISTS FOR THE TREATMENT OF TYPE 2 DIABETES Introduction History Synthesis Mode of Action Structure?Activity Relationship INDEX