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Your search keyword '"Christopher B, Cooper"' showing total 6 results
Start Over Author "Christopher B, Cooper" Journal bioorganic & medicinal chemistry letters
6 results on '"Christopher B, Cooper"'

1. Synthetic approaches towards bedaquiline and its derivatives

Author

Daniel P. Furkert, Christopher B. Cooper, Margaret A. Brimble, and Matthew B. Calvert

Subjects
Drug, Azides, Tuberculosis, media_common.quotation_subject, Clinical Biochemistry, Antitubercular Agents, Drug Evaluation, Preclinical, Pharmaceutical Science, Pharmacology, Selective inhibition, 01 natural sciences, Biochemistry, Catalysis, Structure-Activity Relationship, chemistry.chemical_compound, Diarylquinolines, Tuberculosis, Multidrug-Resistant, Drug Discovery, medicine, Animals, Humans, Molecular Biology, media_common, Cycloaddition Reaction, Molecular Structure, ATP synthase, biology, 010405 organic chemistry, Chemistry, Organic Chemistry, Stereoisomerism, Mycobacterium tuberculosis, Triazoles, medicine.disease, Resistant tuberculosis, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Mechanism of action, Alkynes, biology.protein, Molecular Medicine, medicine.symptom, Bedaquiline
Abstract

Bedaquiline is a diarylquinoline drug that demonstrates potent and selective inhibition of mycobacterial ATP synthase, and is clinically administered for the treatment of multi-drug resistant tuberculosis. Due to its excellent activity and novel mechanism of action, bedaquiline has been the focus of a number of synthetic studies. This review will discuss these synthetic approaches, as well as the synthesis and bioactivity of the numerous derivatives and molecular probes inspired by bedaquiline.

Published
2020

2. Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease

Author

Kristin Kelly, Christopher John Helal, Tate Bonnie Frances, Mavis Diane Adam, Zhijun Kang, Marcia F. Peterson, Thomas G. Gant, Christopher B. Cooper, Michael K. Ahlijanian, Stanley William Kupchinsky, John C. Lucas, Frank S. Menniti, and Sanner Mark Allen

Subjects
Cyclin E, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Nerve Tissue Proteins, Isobutyramide, Pharmacology, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Aminothiazole, Alzheimer Disease, Drug Discovery, CDC2-CDC28 Kinases, Protein kinase A, Molecular Biology, Molecular Structure, biology, Kinase, Cyclin-dependent kinase 5, Cyclin-Dependent Kinase 2, Organic Chemistry, Cyclin-dependent kinase 2, Cyclin-Dependent Kinase 5, Amides, Cyclin-Dependent Kinases, Thiazoles, nervous system, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine
Abstract

High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved.

Published
2004

3. Synthesis and in vitro antibacterial activities of novel conformationally restricted hygromycin a analogues

Author

Christopher S. Jones, Martha L. Minich, Kyle T. Blair, and Christopher B. Cooper

Subjects
Bicyclic molecule, Chemistry, medicine.drug_class, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Biochemistry, Chemical synthesis, Combinatorial chemistry, In vitro, carbohydrates (lipids), Aminocyclitol, chemistry.chemical_compound, Drug Discovery, medicine, Molecular Medicine, Molecular Biology, Hygromycin A, Antibacterial agent
Abstract

The preparation of semisynthetic conformationally restricted hygromycin A analogues are described. Antibacterial results from these compounds suggest active conformations for this class of agents.

Published
1997

4. Synthesis of 1,2,4-triazine-(2H,4H)-3,5,-dione anticoccidial agents via palladium-catalyzed cross-coupling reactions

Author

Kyle T. Blair, Christopher S. Jones, Maria L. Muzzi, Christopher B. Cooper, Edward H. Fontaine, and James W. McFarland

Subjects
Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, chemistry.chemical_element, Cross reactions, Biochemistry, Coupling reaction, Shapiro reaction, Catalysis, chemistry.chemical_compound, Chemical coupling, chemistry, Drug Discovery, Molecular Medicine, Organic chemistry, Molecular Biology, Anticoccidial Agents, Triazine, Palladium
Abstract

Palladium-mediated coupling of 2-(4-iodoaryl)-1,2,4-triazine-(2H,4H)-3,5-diones with variously substituted vinylstannanes has been examined in efforts to explore the SAR of novel triazine anticoccidials. Conventional procedures were employed for the large-scale preparation of key iodoaryltriazine intermediates while a new method - employing a modified Shapiro reaction - was developed for the synthesis of 1,1-substituted vinylstannanes.

Published
1994

5. Synthesis and vitro antibacterial activity of hygromycin a analogs modified at the C4′ aryl position

Author

Douglas L. Schicho, Burton H. Jaynes, Scott J. Hecker, Susan C. Lilley, Kim M. Werner, Christopher B. Cooper, Kyle T. Blair, Martha L. Minich, and Nancy C. Elliott

Subjects
Treponema, biology, Chemistry, Stereochemistry, Aryl, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, biology.organism_classification, Biochemistry, In vitro, carbohydrates (lipids), Minimum inhibitory concentration, chemistry.chemical_compound, Drug Discovery, Molecular Medicine, Antibacterial activity, Molecular Biology, Pathogen, Bacteria, Antibacterial agent
Abstract

A variety of hygromycin A analogs are described which contain modifications of or replacements for the natural sugar. Antibacterial activities against Serpulina (Treponema) hyodysenteriae , an important animal health pathogen, are reported and indicate that small lipophilic C 4′ substituents serve as useful sugar surrogates in the hygromycin A class.

Published
1993

6. Semisynthetic modification of hygromycin A. 2. synthesis and antibacterial activity of aryl analogs

Author

Scott J. Hecker, Martha L. Minich, Kim M. Werner, Kyle T. Blair, Susan C. Lilley, and Christopher B. Cooper

Subjects
Treponema, biology, Animal health, Chemistry, animal diseases, Aryl, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, respiratory system, biology.organism_classification, Biochemistry, Microbiology, carbohydrates (lipids), chemistry.chemical_compound, Drug Discovery, otorhinolaryngologic diseases, Molecular Medicine, Pasteurella multocida, Antibacterial activity, Molecular Biology, Hygromycin A
Abstract

Syntheses of analogs exploring the SAR of the aryl region of hygromycin A are described. Antibacterial activities against Serpulina (Treponema) hyodysenteriae and Pasteurella multocida, two key animal health pathogens, are reported.

Published
1993

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