Bioactive Heterocyclic Compound Classes

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.

AGROCHEMICALS

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: Herbicides

TRIAZINE HERBICIDES
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationships

PYRIMIDINYL AND TRIAZINYLSULFONYLUREA HERBICIDES
Introduction
History
Synthesis
Mode 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
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationship

PYRIDYLOXYPHENOXYPROPIONATE HERBICIDES: INHIBITORS OF ACETYL-COACARBOXYLASE
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationships

IMIDAZOLINONE HERBICIDES
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationship

PROTOPORPHYRINOGEN-IX-OXIDASE-INHIBITING URACIL HERBICIDES
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationship

PART II: Fungicides

BENZIMIDAZOLE 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
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationship

PHENYLPYRAZOLE-CONTAINING FIPROLE INSECTICIDES
Introduction
History
Synthesis
Mode of Action
Biological Activity
Structure - Activity Relationship

PYRAZOLYLPYRIDINE 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

PHARMACEUTICALS

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