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Start Over Author "Chet Lee" Journal bioorganic & medicinal chemistry letters
2 results on '"Chet Lee"'

1. Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists

Author

Chet Lee, E. E. Reynolds, R. Thomas Winters, M. A. Flynn, Annette Marian Doherty, S. Klutchko, Xue-Min Cheng, and Kathleen M. Welch

Subjects
Stereochemistry, Chemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, respiratory system, Selective antagonist, Biochemistry, Endothelin A Receptor Antagonists, Drug Discovery, cardiovascular system, Molecular Medicine, Endothelin receptor, Molecular Biology, circulatory and respiratory physiology
Abstract

Screening of a compound library against endothelin receptors (ETA and ETB) revealed PD 102566 (compound 1) as an ETA selective antagonist. Synthesis and structure-activity relationships (SAR) of a series of analogs are described.

Published
1996
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2. Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

Author

Robert Davis, Mark R. Emmerling, Juan C. Jaen, Vlad E. Gregor, and Chet Lee

Subjects
Aché, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Acetylcholinesterase, language.human_language, Catalysis, chemistry.chemical_compound, chemistry, Tacrine, Drug Discovery, medicine, Quinazoline, language, Molecular Medicine, Potency, Molecule, Molecular Biology, Derivative (chemistry), medicine.drug
Abstract

A new type of dihydroquinazoline-based inhibitor of acetylcholinesterase (AChE) is described. These compounds were designed to interact with the catalytic site of AChE in a manner similar to the known inhibitor tacrine. In a manner analogous to the potency enhancement obtained by addition of chlorine atoms to the tacrine molecule, a 3-chloro derivative of the parent hexahydroazepino[2,1-b]quinazoline structure was found to be about 8 times more potent as an AChE inhibitor than the unsubstituted compound.

Published
1996
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