Pyrazole NNRTIs 3: Optimisation of physicochemical properties

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 19, 2009, Pages 5603-5606

  Mowbray, Charles E ^a   Corbau, Romuald ^a   Hawes, Michael ^a   Jones, Lyn H ^a   Mills, James E ^a   Perros, Manos ^a   Selby, Matthew D ^a   Stupple, Paul A ^a   Webster, Rob ^a   Wood, Anthony ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

HIV; NNRTI; Reverse transcriptase

Indexed keywords

BENZYL DERIVATIVE; EFAVIRENZ; PYRAZOLE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ARTICLE; CHEMICAL MODIFICATION; HUMAN; HUMAN CELL; LIPOPHILICITY; LIVER MICROSOME; PHYSICAL CHEMISTRY; WILD TYPE;

ANTI-HIV AGENTS; DRUG DESIGN; HIV REVERSE TRANSCRIPTASE; HUMANS; MICROSOMES, LIVER; PHYSICOCHEMICAL PROCESSES; PYRAZOLES; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 69949108856     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.08.043     Document Type: Article

References (11)

1. First paper in this series 'Pyrazole NNRTIs 1: Design and Initial Optimization of a Novel Template': Mowbray, C. E.; Burt, C.; Corbau, R.; Perros, M.; Tran, I.; Stupple, P. A.; Webster, R.; Wood A. Bioorg. Med. Chem. Lett. 2009, in press. doi:10.1016/j.bmcl.2009.08.039.
2. The second paper in this series 'Pyrazole NNRTIs 2: Exploring the Dependency of Potency on Lipophilicity': Burt, C.; Corbau, R.; Mills, J.; Mowbray, C. E.; Perros, M.; Tran, I.; Price, D.A.; Selby, M. D.; Stupple, P. A.; Webster, R.; Wood, A. Manuscript in preparation.
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4. The same concept was independently proposed by researchers at Pfizer and termed lipE. Ryckmans, T.; Edwards, M. P.; Horne, V. A.; Monica Correia, A.; Owen, D. R.; Thompson, L. R.; Tran, I.; Tutt, M. F.; Young, T. Bioorg. Med. Chem. Lett. 2009, 15, 4406.
5. Corbau, R. G.; Mowbray, C. E.; Perros, M.; Stupple, P. A.; Wood, A. World Patent Application WO 200204424.
6. Corbau, R. et al. Poster Presentation, 47th Interscience Conference on Antimicrobial Agents and Chemotherapy, September 17-20, 2007, Chicago.
7. Corbau, R. et al. Antimicrob. Agents Chemother. 2009, in press.
8. 4,6 and will be discussed in more detail elsewhere.
9. Jones, L. H.; Mowbray, C. E.; Price, D. A.; Selby, M. D.; Stupple, P. A. World Patent Application WO 2002085860.
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