Bioactive Carboxylic Compound Classes

Pharmaceuticals and Agrochemicals

Lamberth, Clemens / Dinges, Jürgen (Editor)

1. Edition July 2016
XXII, 504 Pages, Hardcover
398 Pictures
Handbook/Reference Book

ISBN: 978-3-527-33947-1

Wiley-VCH, Weinheim

Wiley Online Library Content Sample Chapter Index

Short Description

Following a successful and proven concept developed by the editors, this useful reference is the first to present approved pharmaceutical and agrochemical compounds classified by their carboxylic acid functionality in one handy volume.

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Further versions

Following the successful and proven concept used in "Bioactive Heterocyclic Compound Classes" by the same editors, this book is the first to present approved pharmaceutical and agrochemical compounds classified by their carboxylic acid functionality in one handy volume.
Each of the around 40 chapters describes one or two typical syntheses of a specific compound class and provides concise information on the history of development, mode of action, biological activity and field of application, as well as structure-activity relationships. In addition, similarities and differences between pharmaceuticals and agrochemicals are discussed in the introduction.
Written by a team of experts in the field, this is a useful reference for researchers in academia and chemical or pharmaceutical companies working in the field of total synthesis and natural product chemistry, drug development, and crop protection research.

1. Introduction: Different Roles of Carboxylic Acid Functions in Pharmaceutical and Agrochemical Active Ingredients

PART I: PHARMACEUTICALS
2. Angiotensin II Receptor Antagonistic Acids in Cardiovascular Disease
3. Anti-inflammatory Corticosteroid Esters
4. Non-steroidal Anti-Inflammatory Drugs (NSAIDs)
5. Anticholinergic Muscarinic Receptor Antagonist Esters
6. Oxazolidinone Amide Antibiotics
7. Prostaglandine Analog Esters and Amides for the Treatment of Glaucoma
8. 5a-Reductase Inhibiting Amides
9. Analgesic and Anesthetic Amides
10. Fibrate Acids and Esters in the Treatment of Hyperlipidemia
11. Dipeptidyl Peptidase-4 (DPP-4) Inhibiting Amides
12. NS5B Polymerase Inhibiting Esters (Sovaldi)
13. Dimethyl Fumarate for the Treatment of Multiple Sclerosis
14. Acids for the Treatment of Neuropathic Pain, Anxiety Disorder, and Fibromyalgia (Pregabalin, Lyrica)
15. Factor Xa Inhibiting Amides (Rivaroxaban, Xarelto)
16. Thrombin Inhibiting Esters and Acids
17. Neuraminidase Inhibiting Esters and Acids
18. Carboxylic Acids as Antihistamines
19. Norepinephrine-Dopamine Reuptake Inhibiting Esters (Ndris)
20. Statin HMG Coa Reductase Inhibiting Acids as Hypolipidemic Agents
21. Tyrosine Kinase Inhibiting Amides (Ibrutinib)
22. Chemotherapeutic Acids (Pemetrexed)
23. Platelet Inhibiting Esters for the Reduction of Thrombotic Cardiovascular Events (Prasugrel)
24. TAAR1 Agonist Amides for the Treatment of ADHD (Lisdexamfetamine)

PART II: AGROCHEMICALS

HERBICIDES
25. Amino Acids as Non-Selective Herbicides
26. Herbicidal Esters Inhibiting Protoporphyrinogen Oxidase
27. Herbicidal Chloroacetamides
28. Herbicidal ALS-Inhibiting Imidazolinone Carboxylic Acids
29. Herbicidal Benzoic Acids and Phenoxyacetic Acids as Synthetic Auxins
30. Herbicidal ALS-Inhibiting Sulfonylureas
31. Herbicidal Aryloxyphenoxypropionates (FOPs) Inhibiting Acetyl-Coa Carboxylase

FUNGICIDES
32. Fungicidal Complex III Inhibiting Strobilurin Esters and Amides
33. Fungicidal Succinate Dehydrogenase Inhibiting Carboxamides
34. Fungicidal RNA Polymerase Inhibiting Phenylamides
35. Fungicidal Carboxylic Acid Amide Fungicides Inhibiting Cellulose Synthase
36. Melanin Biosynthesis Inhibiting Amides as Rice Fungicides

INSECTICIDES
37. Insecticidal Pyrethroid Esters
38. Insecticidal Juvenile Hormone Analog Esters
39. Chitin Biosynthesis Inhibiting Benzoylureas
40. Ecdyson Receptor Agonistic Diacylhydrazine Insecticides
41. Acetyl Coa Esterase Inhibiting Tetramic and Tetronic Acid Procide Esters and Carbonates
42. Ryanodine Receptor Modulating Diamides

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 he joined the agrochemical research department of Sandoz Agro AG, Switzerland, which is today, after two mergers, part of Syngenta Crop Protection AG. Since 22 years he is specialized in fungicide discovery. He is the author of more than 130 publications and patents and inventor of Syngenta's fungicide mandipropamid (Revus®, Pergado®).

Jürgen Dinges is a senior principal research scientist in the pharmaceutical research department at Abbvie, USA. He studied chemistry at the Technical University of Darmstadt, Germany, where he obtained his Ph.D. degree in organic chemistry and chemical engineering under the supervision of Prof. Frieder W. Lichtenthaler 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 he joined the Department for Biochemistry at Syntex, USA, which today is part of Hoffmann-La Roche Ltd., Switzerland. In 1995 he joined the pharmaceutical research department at Abbott Laboratories, USA, which became part of Abbvie in 2013. Since 19 years he is specialized in drug discovery. He is an author on 57 publications and patents and a co-inventor of more than 10 clinical drug development candidates.

C. Lamberth, Syngenta Crop Protection AG, Stein, Switzerland; J. Dinges, Syngenta Crop Protection AG, Stein, Switzerland