Affiliation: Merck Research Laboratories
- 2-Aryl indole NK(1) antagonists: optimisation of the amide substituentD Shaw
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
Bioorg Med Chem Lett 11:3031-4. 2001..Replacement of this amine moiety by a 4-benzyl-4-hydroxypiperidine resulted in a compound 18 with reduced clearance and improved central duration of action...
- 3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitorsDuncan Shaw
Department of Medicinal Chemistry, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
Bioorg Med Chem Lett 16:3073-7. 2006....
- Drug-resistant variants of Escherichia coli thymidylate synthase: effects of substitutions at Pro-254C Fantz
Department of Chemistry, Columbia, South Carolina, USA
Mol Pharmacol 57:359-66. 2000..When compared with wild-type TS, the structure shows local conformational changes affecting mostly Asp-253; its carbonyl is rotated approximately 40 degrees, and the side chain forms an ion pair with Arg-225...