Bioactive Heterocyclic Compound Classes, 2 Vols. - Pharmaceuticals and Agrochemicals

Filling a gap in the market, this two-volume set is the first to present important pharmaceuticals as well as agrochemical pesticides in one handy work.Each of the around 40 chapters covers in a concise manner one class of heterocycles, clearly structured as 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 field of pharmaceutical and agrochemical chemistry.

List of contents

AGROCHEMICALSTHE SIGNIFICANCE OF HETEROCYCLES FOR PHARMACEUTICALS AND AGROCHEMICALS Introduction Heterocycles as Framework of Biologically Active Compounds Fine-Tuning the Physicochemical Properties with Heterocycles Heterocycles as ProdrugsHeterocycles 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: Herbicides TRIAZINE HERBICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationships PYRIMIDINYL AND TRIAZINYLSULFONYLUREA HERBICIDES Introduction History SynthesisMode of Action Biological Activity Structure - Activity Relationship ACETOHYDROXYACID SYNTHASE INHIBITING TRIAZOLOPYRIMIDINE HERBICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship HPPD-INHIBITING BENZOYLPYRAZOLE HERBICIDES IntroductionHistory Synthesis Mode of Action Biological Activity Structure - Activity Relationship PYRIDYLOXYPHENOXYPROPIONATE HERBICIDES: INHIBITORS OF ACETYL-COACARBOXYLASE Introduction History Synthesis Mode of ActionBiological Activity Structure - Activity Relationships IMIDAZOLINONE HERBICIDES Introduction History Synthesis Mode of ActionBiological Activity Structure - Activity Relationship PROTOPORPHYRINOGEN-IX-OXIDASE-INHIBITING URACIL HERBICIDES Introduction History Synthesis Mode of ActionBiological Activity Structure - Activity Relationship PART II: FungicidesBENZIMIDAZOLE FUNGICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship MORPHOLINE FUNGICIDES FOR THE TREATMENT OF POWDERY MILDEW Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship STEROL BIOSYNTHESIS INHIBITING TRIAZOLE FUNGICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship METHIONINE BIOSYNTHESIS-INHIBITING ANILINOPYRIMIDINE FUNGICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship PHENYLPYRROLE FUNGICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship BROAD-SPECTRUM FUNGICIDALLY ACTIVE PYRIMIDINYLDIOXY STROBILURINS INHIBITING THE RESPIRATORY CHAIN Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship PYRAZOLE CARBOXAMIDE FUNGICIDES INHIBITING SUCCINATE DEHYDROGENASE Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationships PART III: Insecticides AVERMECTIN INSECTICIDES AND ACARICIDES Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship PYRIDINE AND THIAZOLE-CONTAINING INSECTICIDES AS POTENT AGONISTS ON INSECT NICOTINIC ACETYLCHOLINE RECEPTORS Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship PYRAZOLE AND PYRIMIDINE ACARICIDES AND INSECTICIDES ACTING AS INHIBITORS OF MITOCHONDRIAL ELECTRON TRANSPORT AT COMPLEX I IntroductionHistory Synthesis Mode of Action Biological Activity Structure - Activity Relationship PHENYLPYRAZOLE-CONTAINING FIPROLE INSECTICIDES Introduction History SynthesisMode of Action Biological Activity Structure - Activity RelationshipPYRAZOLYLPYRIDINE ACTIVATORS OF THE INSECT RYANODINE RECEPTOR Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationships TETRONIC ACID INSECTICIDES AND ACARICIDES INHIBITING ACETYL-COACARBOXYLASE Introduction History Synthesis Mode of Action Biological Activity Structure - Activity Relationship PHARMACEUTICALSTHE 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 RingsHeterocycles as Isosteric Replacement of other Heterocyclic RingsPART I: Neurological DisordersTROPANE-BASED ALKALOIDS AS MUSCARINIC ANTAGONISTS FOR THE TREATMENT OF ASTHMA, OBSTRUCTIVE PULMONARY DISEASE, AND MOTION SICKNESSIntroduction 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 SCHIZOPHRENIAIntroduction 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 SCHIZOPHRENIAIntroduction 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 SynthesisMode 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 AGENTSIntroduction History Synthesis Mode of Action Structure - Activity RelationshipGUANINE-BASED NUCLEOSIDE ANALOGS AS ANTIVIRAL AGENTS Introduction HistorySynthesis Mode of Action Structure - Activity Relationship PENICILLIN AND CEPHALOSPORIN ANTIBIOTICS Introduction History Synthesis Mode of Action Structure - Activity RelationshipsPART 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 EYEIntroduction 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 ActionStructure - Activity Relationships PART VI: Metabolic DiseasesTHIAZOLIDINEDIONE-BASED INSULIN SENSITIZERS:PPAR-G AGONISTS FOR THE TREATMENT OF TYPE 2 DIABETES Introduction History Synthesis Mode of Action Structure - Activity Relationship

About the author

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 (USA). 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, Italy, 2008. He is the author of 46 publications and 56 patents and the inventor of Syngenta's fungicide mandipropamid (Revus®, Pergado®).

Jürgen 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 (USA). In 1993, Jürgen Dinges joined the department for biochemistry at Syntex, USA and since 1995 he is working in the pharmaceutical research department at Abbott Laboratories, USA. During his 18 years of industrial experience, Jürgen Dinges has specialized in drug discovery. 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.

Summary

Filling a gap in the market, this two-volume set is the first to present important pharmaceuticals as well as agrochemical pesticides in one handy work.
Each of the around 40 chapters covers in a concise manner one class of heterocycles, clearly structured as 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 field of pharmaceutical and agrochemical chemistry.

Product details

• Authors: Jürgen Dinges, Clemens Lamberth
• Assisted by: Dinges (Editor), Dinges (Editor), Jürgen Dinges (Editor), Clemen Lamberth (Editor), Clemens Lamberth (Editor)
• Publisher: Wiley-VCH
• Languages: English
• Product format: Mixed media product
• Released: 01.09.2012
• EAN: 9783527329939
• ISBN: 978-3-527-32993-9
• No. of pages: 670
• Weight: 1582 g
• Subjects: Natural sciences, medicine, IT, technology > Chemistry > Organic chemistry; Chemie, Biochemie, Organische Chemie, ORGANIC CHEMISTRY, Life Sciences, Biowissenschaften, biochemistry, chemistry, Natural Products, Naturstoffchemie, Pharmaceutical & Medicinal Chemistry, Pharmazeutische u. Medizinische Chemie, PHARMAZEUTISCHE CHEMIE, Agrochemikalien, Agrochemicals, Heterocyclische Verbindungen, Agrochemikalie, Bioaktive Verbindungen