Pyrrolidine-5,5-trans-lactams.: 2.: The use of X-ray crystal structure data in the optimization of P3 and P4 substituents

被引：15

作者：

Andrews, DM ^{[1
]}

Chaignot, H ^{[1
]}

Coomber, BA ^{[1
]}

Good, AC ^{[1
]}

Hind, SL ^{[1
]}

Johnson, MR ^{[1
]}

Jones, PS ^{[1
]}

Mills, G ^{[1
]}

Robinson, JE ^{[1
]}

Skarzynski, T ^{[1
]}

Slater, MJ ^{[1
]}

Somers, DO ^{[1
]}

机构：

[1] GlaxoSmithKline Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

ORGANIC LETTERS | 2002年 / 4卷 / 25期

关键词：

D O I：

10.1021/ol027014p

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] 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.

引用

页码：4479 / 4482

页数：4

共 17 条

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