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Your search keyword '"Pickford, Christopher"' showing total 2 results
Start Over Author "Pickford, Christopher" Journal bioorganic medicinal chemistry letters
2 results on '"Pickford, Christopher"'

1. Design and optimisation of potent gp120-CD4 inhibitors.

Author

Tran TD, Adam FM, Calo F, Fenwick DR, Fok-Seang J, Gardner I, Hay DA, Perros M, Rawal J, Middleton DS, Parkinson T, Pickford C, Platts M, Randall A, Stephenson PT, Vuong H, and Williams DH

Subjects
Animals, Cells, Cultured, Drug Design, HIV Envelope Protein gp120 metabolism, HIV Fusion Inhibitors chemical synthesis, HIV Fusion Inhibitors pharmacokinetics, HIV-1 drug effects, Half-Life, Humans, Isoquinolines chemical synthesis, Isoquinolines pharmacokinetics, Nicotinic Acids chemical synthesis, Nicotinic Acids pharmacokinetics, Rats, Structure-Activity Relationship, CD4 Antigens metabolism, HIV Envelope Protein gp120 antagonists & inhibitors, HIV Fusion Inhibitors chemistry, Isoquinolines chemistry, Nicotinic Acids chemistry
Abstract

The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.

Published
2009
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2. Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction.

Author

Williams DH, Adam F, Fenwick DR, Fok-Seang J, Gardner I, Hay D, Jaiessh R, Middleton DS, Mowbray CE, Parkinson T, Perros M, Pickford C, Platts M, Randall A, Siddle D, Stephenson PT, Tran TD, and Vuong H

Subjects
Animals, Biological Availability, Cell Line, Tumor, Drug Design, HIV Envelope Protein gp120 metabolism, HIV Fusion Inhibitors chemical synthesis, HIV Fusion Inhibitors pharmacokinetics, HIV-1 drug effects, Humans, Microsomes, Liver metabolism, Piperazines chemical synthesis, Piperazines pharmacokinetics, Rats, Structure-Activity Relationship, CD4 Antigens metabolism, HIV Envelope Protein gp120 antagonists & inhibitors, HIV Fusion Inhibitors chemistry, Piperazines chemistry
Abstract

A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.

Published
2009
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