Pyrrolidine-5,5-trans-lactams. 2. The Use of X-ray Crystal Structure Data in the Optimization of P3 and P4 Substituents

In this, the second of two letters, we describe the elaboration of the pyrrolidine-5,5-trans-lactam template to delineate the requirements for optimal substitution of the pyrrolidine and lactam nitrogen atoms. Central to the strategy is the use of rapid iterative synthesis in conjunction with X-ray...

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Veröffentlicht in:	Organic letters 2002-12, Vol.4 (25), p.4479-4482
Hauptverfasser:	Andrews, David M, Chaignot, Helene, Coomber, Barry A, Good, Andrew C, Hind, S. Lucy, Johnson, Martin R, Jones, Paul S, Mills, Gail, Robinson, J. Ed, Skarzynski, Tadeusz, Slater, Martin J, Somers, Donald O'N
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Hepacivirus - drug effects Hepacivirus - enzymology Inhibitory Concentration 50 Lactams - chemical synthesis Lactams - chemistry Lactams - pharmacology Models, Molecular Molecular Structure Protein Conformation Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - chemistry Viral Nonstructural Proteins - metabolism
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Zusammenfassung:	In this, the second of two letters, we describe the elaboration of the pyrrolidine-5,5-trans-lactam template to delineate the requirements for optimal substitution of the pyrrolidine and lactam nitrogen atoms. Central to the strategy is the use of rapid iterative synthesis in conjunction with X-ray crystal structure determination of ligand−protein complexes.
ISSN:	1523-7060 1523-7052
DOI:	10.1021/ol027014p