Genomes and Genes
Alan H Katz
Affiliation: Wyeth Research
- Structure-based design approaches to cell wall biosynthesis inhibitorsAlan H Katz
Wyeth Ayerst Research, Princeton, NJ 08540, USA
Curr Pharm Des 9:857-66. 2003..For example, mutations within the d-Ala-d-Ala ligases lead to the inability of Vancomycin antibiotics to bind...
- 4-Alkyl and 4,4'-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesisKristina M K Kutterer
Wyeth Research, Chemical and Screening Sciences, 401 N Middletown Rd, Pearl River, NY 10965, USA
Bioorg Med Chem Lett 15:2527-31. 2005..Derivative 7l demonstrated antibacterial activity against both gram-positive and gram-negative bacteria. Derivatives 7f and 10a also demonstrated potent nanomolar Kd values in their binding to MurB...
- Identification and characterization of small molecule modulators of KChIP/Kv4 functionMark R Bowlby
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Bioorg Med Chem 13:6112-9. 2005..Molecular modeling using the KChIP1 crystal structure indicates that compound binding may occur in a small tryptophan-containing binding pocket located on the hydrophilic side of the protein...
- Use of a murine cell line for identification of human nitric oxide synthase inhibitorsSaule Naureckiene
Neuroscience Discovery Research, Wyeth Research, CN8000, Princeton, NJ 08543, USA
J Pharmacol Toxicol Methods 55:303-13. 2007..This upregulation is due in part to the induction of inducible nitric oxide synthase (iNOS) by proinflammatory cytokines in several different cell types, including macrophages and their CNS derivative, microglia...
- Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductaseAdam M Gilbert
Chemical and Screening Sciences and Infectious Diseases Research, Wyeth, 401 North Middletown Road, Pearl River, New York 10965, USA
J Med Chem 49:6027-36. 2006..Docking studies using FLO and PharmDock produced several binding orientations for these molecules in the MurB active site...
- Two N-terminal domains of Kv4 K(+) channels regulate binding to and modulation by KChIP1Robert H Scannevin
Neuroscience Discovery Research, Wyeth Research CN 8000, Princeton, NJ 08543, USA
Neuron 41:587-98. 2004....
- Modeling G protein-coupled receptors for structure-based drug discovery using low-frequency normal modes for refinement of homology models: application to H3 antagonistsBrajesh K Rai
Wyeth Research, CN8000, Princeton, New Jersey 08543 8000, USA
Proteins 78:457-73. 2010....
- Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesisGerardo D Francisco
Chemical Sciences and Infectious Diseases, Wyeth Research, Pearl River, NY 10965, USA
Bioorg Med Chem Lett 14:235-8. 2004..3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria...