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Your search keyword '"Nicholas K. Terrett"' showing total 2 results
Start Over Author "Nicholas K. Terrett" Journal bioorganic & medicinal chemistry letters
2 results on '"Nicholas K. Terrett"'

1. Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction

Author

Peter M. Ellis, Brown David Graham, Nicholas K. Terrett, and Andrew Simon Bell

Subjects
Oral treatment, Chemistry, Sildenafil, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Drug design, Phosphodiesterase, Male erectile dysfunction, Pharmacology, Biochemistry, respiratory tract diseases, chemistry.chemical_compound, Drug Discovery, cardiovascular system, Molecular Medicine, Platelet, Molecular Biology
Abstract

5-(2′-Alkoxyphenyl)pyrazolo[4,3-d]pyrimidin-7-ones, and in particular our preferred compound, sildenafil (VIAGRATM), discovered through a rational drug design programme, are potent and selective inhibitors of the type 5 cGMP phosphodiesterase from both rabbit platelets and human corpus cavernosum. Sildenafil is currently in the clinic for the oral treatment of male erectile dysfunction.

Published
1996

2. The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317

Author

Carolyn J. Mayers, M. J. Gardner, David G. Brown, Nicholas K. Terrett, Dejan Bojanic, Peter J. Bungay, John Steele, and David W. Gordon

Subjects
chemistry.chemical_classification, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Antagonist, Pharmaceutical Science, Positive control, Combinatorial synthesis, Biochemistry, Combinatorial chemistry, Amino acid, chemistry, Drug Discovery, Molecular Medicine, Endothelin receptor, Molecular Biology
Abstract

A combinatorial library of 30,752 compounds has been synthesised from a set of 32 natural and unnatural amino acids. The library was designed to include the known endothelin antagonist, FR-139,317, as a positive control, and this and a number of close analogues were shown to be the most potent compounds. Thus, combinatorial libraries may be used both to discover leads and rapidly explore SAR. A combinatorial library of 30,752 compounds has been synthesised from a set of 32 natural and unnatural amino acids. The library was designed to include the known endothelin antagonist, FR-139,317, as a positive control, and this and a number of close analogues were shown to be the most potent compounds. Thus, combinatorial libraries may be used both to discover leads and rapidly explore SAR.

Published
1995

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