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Your search keyword '"Hannah Vuong"' showing total 3 results
Start Over Author "Hannah Vuong" Topic pharmaceutical science
3 results on '"Hannah Vuong"'

1. Discovery of a small molecule inhibitor through interference with the gp120–CD4 interaction

Author

Rawal Jaiessh, Amy Randall, Tram T. Tran, Fiona M. Adam, Daniel Siddle, Iain Gardner, Tanya Parkinson, Manos Perros, David R. Fenwick, Christopher Pickford, Juin Fok-Seang, Charles E. Mowbray, David Howard Williams, Donald Stuart Middleton, Hannah Vuong, Peter T. Stephenson, Michelle Y. Platts, and Duncan Hay

Subjects
medicine.drug_class, Stereochemistry, Clinical Biochemistry, Biological Availability, Pharmaceutical Science, Ether, Carboxamide, HIV Envelope Protein gp120, Biochemistry, Chemical synthesis, Piperazines, Structure-Activity Relationship, chemistry.chemical_compound, Viral envelope, HIV Fusion Inhibitors, Cell Line, Tumor, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Molecular Biology, Organic Chemistry, Small molecule, In vitro, Rats, Piperazine, chemistry, Drug Design, CD4 Antigens, HIV-1, Microsomes, Liver, Molecular Medicine
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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2. Design and optimisation of potent gp120-CD4 inhibitors

Author

Jaiessh Rawal, David Howard Williams, Donald Stuart Middleton, Michelle Y. Platts, Juin Fok-Seang, Manos Perros, Frederick Calo, Duncan Hay, Christopher Pickford, David R. Fenwick, Tram T. Tran, Hannah Vuong, Fiona M. Adam, Iain Gardner, Tanya Parkinson, Peter T. Stephenson, and Amy Randall

Subjects
medicine.drug_class, Clinical Biochemistry, Human immunodeficiency virus (HIV), Pharmaceutical Science, Carboxamide, HIV Envelope Protein gp120, medicine.disease_cause, Biochemistry, Chemical synthesis, Virus, Structure-Activity Relationship, In vivo, HIV Fusion Inhibitors, Drug Discovery, medicine, Structure–activity relationship, Potency, Animals, Humans, Molecular Biology, Cells, Cultured, Chemistry, Organic Chemistry, Nicotinic Acids, Isoquinolines, In vitro, Rats, Drug Design, CD4 Antigens, HIV-1, Molecular Medicine, Half-Life
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

3. Discovery of an HIV integrase inhibitor with an excellent resistance profile

Author

Ieuan O. Roberts, Kevin Whitby, Mike Westby, Darren Stead, Claire Bru, David John Bull, Richard A. Bissell, Edward J. Murray, Chris Pickford, Michael John Palmer, David C. Blakemore, Wai-Yee Cheung, Iain Gardner, Christopher P. Ashcroft, David C. Pryde, Rob Webster, Hannah Vuong, Jennifer Morton, and Scott L. Butler

Subjects
Pharmacology, biology, Organic Chemistry, Pharmaceutical Science, Biochemistry, Virology, Integrase, Pharmacokinetics, MicroDose, Drug Discovery, biology.protein, HIV Integrase Inhibitors, Molecular Medicine, Potency
Abstract

In the present article, we describe SAR studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors that led to a candidate compound, PF-4776548, of high potency and with an excellent resistance profile. Uncertainties around the human pharmacokinetic predictions for PF-4776548 led to the compound being taken into a human microdose study to confirm its human pharmacokinetics, the results of which are described herein.

Published
2013
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