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Pyrrolidine-5,5-trans-lactams. 2. The use of X-ray crystal structure data in the optimization of P3 and P4 substituents |
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| Authors: | 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 |
| Affiliation: | GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, UK. david.m.andrews@gsk.com |
| Abstract: | [reaction: see text] 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. |
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